Generic peptides

We manufacture high-quality GMP Generic Peptides

BCNpeptides manufactures under strict GMP conditions a large number of generic peptide API at commercial scale for pharmaceutical and veterinary applications. They can be used in different areas such as: oncology, metabolic, reproduction and many more.

Our Generic Peptides are supported by regulatory filing in their respective markets and BCN Peptides will fully support you with the required documentation, including DMFs and CEPs, as BCN Peptides holds Approval status in US FDA, EMEA, and PMDA among many other national authorities.

Moreover, BCN Peptides is supplier of bulk material for the EU and USP Pharmacopoeias and it also participates in the collaborative studies of both Pharmacopoeias to establish the content of their Standards.

a
ACHT

CAS number:
9002-60-2

Sequence
H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu-Leu-Ala-Glu-Ala-Phe-Pro-Leu-Glu-Phe-OH

Molecular formula: C210H314N56O57S

Molecular weight: 4567.21 a.m.u.

Fields of Application
Diagnosis of adrenocortical insufficiency
As alternative to systemic corticosteroid therapy

Description
Adrenocorticotropic hormone (ACTH), also known as corticotropin, is a polypeptide tropic hormone produced and secreted by the anterior pituitary gland. It is the major regulator of the adrenal cortex function. It is an important component of the hypothalamic-pituitary-adrenal axis and is often produced in response to biological stress (along with its precursor corticotropin-releasing hormone from the hypothalamus). Its principal effects are increased production and release of corticosteroids. A deficiency of ACTH is a cause of secondary adrenal insufficiency and an excess of it is a cause of Cushing’s syndrome.

Administration:
Regular injectable form.

 

Abaloparatide

CAS number:
247062-33-5

Sequence:
H-Ala-Val-Ser-Glu-His-Gln-Leu-Leu-His-Asp-Lys-Gly-Lys-Ser-Ile-Gln-Asp-Leu-Arg-Arg-Arg-Glu-Leu-Leu-Glu-Lys-Leu-Leu-Aib-Lys-Leu-His-Thr-Ala-NH2

Molecular formula: C174H300N56O49

Molecular weight: 3959.65 a.m.u.

Fields of Application: Treatment of osteoporosis
Administration:
Regular injectable form.

Description
Abaloparatide is a 34 amino acid synthetic analog of a parathyroid hormone-related protein (PTHrP), medication used to treat osteoporosis. It is an anabolic (i.e., bone growing) agent and is also used to treat postmenopausal osteoporosis.

Afamelanotide

CAS number: 
75921-69-6

Sequence

Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2

Molecular formula: C78H111N21O19

Molecular weight: 1646.8 a.m.u.

Fields of Application
Phototoxicity

Description
Afamelanotide is  is a synthetic and α-melanocyte stimulating hormone. It has been used to prevent phototoxicity (skin damage) from the sun in people with erythropoietic protoporphyria (EPP).

Administration:
Subcutaneous implant.

Alarelin

CAS number: 
52435-06-0 (net)
79561-22-1 (acetate)

Sequence
Pyr-His-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-NHCH2CH3

Molecular formula: C56H78N16O12

Molecular weight: 1167.35 a.m.u.

Fields of Application
Veterinary: Several activities have been described, like induction of ovulation.

Description
Alarelin is a synthetic polypeptide which acts as LH-RH (Luteinizing-hormone releasing hormone) analogue agonist. LH-RH is secreted in the hypothalamus and its release induces the secretion of LH (Luitenizing hormone) and FSH (Follicle-stimulating hormone) from the pituitary gland. These two hormones act on the ovaries and the testes and are responsible of the profertility effects of LHRH through the release of steroideal hormones.

The biological activity of Alarelin, a synthetic LH-RH agonist, is dozens of times higher than that of LH-RH in the test of rat hypophyseal stimulation of gonadotropin secretion in vivo and in vitro and in the ovulation induction test.

Administration:
Regular injectable form.

Angiotensin I

CAS number:
9041-90-1

Sequence
H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-OH

Molecular formula: C62H89N17O14

Molecular weight: 1296.5 a.m.u.

Fields of Application
Angiotensin II precursor

Description
Angiotensin I, officially called proangiotensin, is a ten amino acid peptide formed by renin cleavage of angiotensinogen. Angiotensin I has no direct biological function except that it is metabolized to its biologically active byproduct angiotensin II, a potent vasoconstrictor, by angiotensin converting enzyme (ACE) through cleavage of the two terminal amino acids. It has a role as a neurotransmitter agent and a human metabolite.

Administration:
Injectable form.

Angiotensin II

CAS number:
4474-91-3

Sequence
H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-OH

Molecular formula: C50H71N13O12

Molecular weight: 1046.2 a.m.u.

Fields of Application
Sepsis
Septic Shock
Diabetes Mellitus
Acute Renal Failure

Description
Angiotensin II is a vasoconstrictor used to increase blood pressure in adults with septic or other distributive shock. Angiotensin II is a naturally occurring hormone secreted as part of the renin-angiotensin system that results in powerful systemic vasoconstriction.

Administration:
Injectable form.

Arginine Vasopressin

CAS number: 
113-79-1

Sequence
Cyclo(1-6)Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH2

Molecular formula: C46H65N15O12S2

Molecular weight: 1084.2 a.m.u.

Fields of Application
Central diabetes insipidus
Oesophageal varices
Cardiopulmonary resuscitation

Description
Arginine Vasopressin is a form of vasopressin obtained from most of mammals including man but excluding pig. It is usually prepared synthetically.

It has a direct antidiuretic action on the kidney, increasing tubular reabsortion of water. It also constricts peripheral blood vessels and causes contraction of the smooth muscle of the intestine, gallbladder and urinary bladder.

Administration:
Regular injectable form and Nasal spray.

Atosiban

CAS number:
90779-69-4

Sequence
3-Mercaptopropionyl-D-Tyr(Et)-Ile-Thr-Asn-Cys-Pro-Orn-Gly-NH2

Molecular formula: C43H67N11O12S2

Molecular weight: 994.20 a.m.u.

Fields of Application
Treat a pre-term labour
Induce a delayed labour
Help prevent excessive blood loss after caesarean section

Description
Atosiban is an inhibitor of the hormones oxytocin and vasopressin. It is used as a labour repressant (tocolytic) to halt premature labor. As an oxytocin/vasopressin antagonist, Atosiban blocks the action of oxytocin and is able to prevent uterine contractions and relax the uterus.

Administration:
Regular injectable form.

b
Bremelanotide

CAS number:
189691-06-3

Sequence
Ac-Nle-Asp(1)-His-D-Phe-Arg-Trp-Lys(1)-OH

Molecular formula: C50H68N14O10

Molecular weight: 1025.2 a.m.u.

Fields of Application
Hypoactive sexual desire disorder (HSDD) in premenopausal women

Description
Bremelanotide is a cyclic heptapeptide lactam analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide acts by activating the melanocortin receptors.

Administration:
Regular injectable form.

Buserelin

CAS number: 
57982-77-1 (net)
68630-75-1 (acetate)

Sequence
Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NH-CH2-CH3

Molecular formula: C60H86N16O13

Molecular weight: 1239.5 a.m.u.

Fields of Application
Prostate Cancer and Endometriosis
Uterine fibroids
Reproduction
Precocious central puberty
Veterinary: Induction of ovulation (cows, mares and rabbits)
Treatment of ovarian disorders

Description
Buserelin is a synthetic nonapeptide analogue of human Gonatropin-releasing hormone (LH-RH) with agonistic activity to gonadorelin.

It is used to treat cancer of the prostate gland. Intranasal and subcutaneous buserelin have demonstrated efficacy in a variety of conditions, including endometriosis, uterine leiomyoma, advanced prostate cancer, polycystic ovary syndrome, central precocious puberty. It has also enhanced success rates of in-vitro fertilization programs. However, comparative trials with other LH-RH analogs (e.g. leuprolide, goserelin) are necessary to establish the place in therapy of buserelin.

Administration:
Regular injectable form and Nasal spray.

c
Carbetocin

CAS number: 
37025-55-1

Sequence
Cyclo(1-6)Butyryl-Tyr(OMe)-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2C45H69N11O12S

Molecular formula: C45H69N11O12S

Molecular weight: 988.2 a.m.u.

Fields of Application
Prevention of bleeding after caesarean
Induction of milk production
Veterinary:  Induction of milk production

Description
Carbetocin is an oxytocin analogue with modifications in the terminal Cysteine residue and in the disulphur bridge betwen Cys1 and Cys6. Carbetocin lacks cysteine residue in position 1, the disulphur has been substituted by a thioether linkage and the phenolic alcohol is blocked by a methyl ether.

It is reported that Carbetocin has a longer duration of action than Oxytocin. It is used for the prevention of uterine atony and excessive bleeding following caesarean.

It is also sometimes used to help milk secretion in breast-feeding.

Carbetocin is also used in veterinary medicine.

Administration:
Regular injectable form.

Carperitide

CAS number:
89213-87-6

Sequence
H-Ser-Leu-Arg-Arg-Ser-Ser-Cys(1)-Phe-Gly-Gly-Arg-Met-Asp-Arg-Ile-Gly-Ala-Gln-Ser-Gly-Leu-Gly-Cys(1)-Asn-Ser-Phe-Arg-Tyr-OH

Molecular formula: C127H203N45O39S3

Molecular weight: 3080.5 a.m.u.

Fields of Application
Acute Heart Failure

Description
Carperitide (alpha-human atrial natriuretic peptide) improves systemic hemodynamics in patients with heart failure through a vasodilatory action, a natriuretic action, and inhibition of the renin-angiotensin-aldosterone system.

Administration:
Injectable form.

d
Desmopressin

CAS number:
16679-58-6 (net)
62288-83-9 (acetate)

Sequence
Cyclo(1-6)Mpa-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH2

Molecular formula: C46H64N14O12S2

Molecular weight: 1069.24 a.m.u.

Fields of Application
Nocturnal enuresis
Central diabetes insipidus, polyuria, polydipsia
Mild and moderate forms of hemophilia A and von Willebrand disease

 

Description
Desmopressin (acetate) is a synthetic analogue of Vasopressin which is a well known neurohypophyseal antidiuretic hormone. Vasopressin can be found in the mammalian kidney where it regulates water reabsorption in the collecting tubules and salt transport. The substitution of the amino terminal Cys residue by mercaptopropanoic acid together with the change in configuration in Arg8, confer to desmopressin an enhanced antidiuretic efficacy and a reduced pressor potency compared with those of vasopressin.

Desmopressin is taken through the nose, by mouth, or given by injection to prevent or control the frequent urination, increased thirst, and loss of water associated with diabetes insipidus (water diabetes).

It is used also to control bed-wetting and frequent urination and increased thirst associated with certain types of brain injuries or brain surgery. Desmopressin works by acting on the kidneys to reduce the flow of urine.

Desmopressin is also given by injection to treat some patients with certain bleeding problems such as hemophilia or von Willebrand’s disease.

Administration:
Regular injectable form, Nasal spray and Oral tablets.

e
Elcaltonin

CAS number: 
60731-46-6

Sequence
Cyclo(-Ser-Asn-Leu-Ser-Thr-Asu)-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asp-Val-Gly-Ala-Gly-Thr-Pro-NH2

Molecular formula: C148H244N42O47

Molecular weight: 3363 a.m.u.

Fields of Application
Osteoporosis
Hypercalcemia
Paget’s disease

Description
Elcaltonin is a synthetic polypeptide analogue of salmon calcitonin I. It lowers the calcium concentration in plasma of mammals by diminishing the rate of bone resorption. It prevents the release of calcium and phosphorous into blood by inhibiting the osteoclasts, a cell type that “digests” bone matrix.

It is obtained by chemical synthesis and it is available as acetate.

Calcitonins are used to treat severe hypercalcemia of various origins, Paget’s disease, osteoporosis of various origins, and intractable cancer pain in patients with malignant bone metastases.

Administration:
Nasal Spray.

Eledoisin

CAS number: 
69-25-0 (net)
10129-92-7 (acetate)

Sequence
Pyr-Pro-Ser-Lys-Asp-Ala-Phe-Ile-Gly-Leu-Met-NH2

Molecular formula: C54H85N13O15S

Molecular weight: 1188.4 a.m.u.

Fields of Application
Dry eye
Sjogren’s syndrome

Description
Eledoisin is a synthetic peptide originally found in the posterior salivary glands of certain small octopi (Eledone spp., Mollusca). It’s actions resemble those of Substance P; it is a potent vasodilator and increases capillary permeability. It has been given as eye drops to stimulate lachrymal secretion in Sjogren’s syndrome and other dry eye conditions.

Administration:
Eye drops.

Etelcalcetide

CAS number:
1262780-97-1

Sequence
Ac-D-Cys(1)-D-Ala-D-Arg-D-Arg-D-Arg-D-Ala-D-Arg-NH2.H-Cys(1)-OH

Molecular formula: C38H73N21O10S2

Molecular weight: 1048.3 a.m.u.

Fields of Application
Secondary hyperparathyroidism in patients with chronic kidney disease (CKD) undergoing hemodialysis

Description
Etelcalcetide is a calcimimetic and calcium-sensing receptor (CaSR) agonist composed of a synthetic peptide comprised of seven D-amino acids. Etelcalcetide mimics calcium and allosterically binds to and activates the CaSR expressed by the parathyroid gland. This suppresses the synthesis and secretion of parathyroid hormone (PTH), thereby reducing PTH levels and lowering serum calcium and phosphorus levels. Elevated PTH is often observed in patients with CKD and is associated with dysregulated calcium-phosphate homeostasis.

Administration:
Injectable form.

 

f
Fertirelin

CAS number:
38234-21-8 (net)
66002-66-2 (acetate)

Sequence:
5-oxoPro-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-NHCH2CH3

Molecular formula: C55H76N16O12

Fields of Application

Veterinary:

Ovarian follicular cysts in cattle

Induction of ovulation

 

Description
Fertirelin is a luteinizing hormone-releasing hormone (LHRH) agonist intended for the treatment of ovarian follicular cysts in cattle and for the improvement of conception rates in this species.

In laboratory species and food producing animals, fertirelin is rapidly excreted and metabolised. The half-life in mammalian species is measured in minutes. In the target species, cattle, there was no accumulation of residues in edible tissues. It is not orally bioavailable and moreover the major metabolites are likely to be naturally occurring aminoacids arising as a result of enzymatic breakdown in the gastrointestinal tract.

Administration:
Regular injectable form.

g
GHRP-6

CAS number:
87616-84-0

Sequence
H-His-D-Trp-Ala-Trp-D-Phe-Lys-NH2

Molecular formula: C46H56N12O6

Molecular weight: 873 a.m.u.

Fields of Application
Diagnostic agent for growth hormone secretion deficiency

Description
Growth hormone-releasing peptide 6 (GHRP-6), also known as growth hormone-releasing hexapeptide, is one of several synthetic met-enkephalin analogues that were developed for their growth hormone-releasing activity and are called growth hormone secretagogues. They lack opioid activity but are potent stimulators of growth hormone (GH) release.

Administration:
Injectable form.

Ganirelix

CAS number:
124904-93-4 (net)
129311-55-3 (acetate)

Sequence:
Ac-D-2Nal-D-Phe(4-Cl)-D-3Pal-Ser-Tyr-D-hArg(Et,Et)-Leu-hArg(Et,Et)-Pro-D-Ala-NH2.2CH3CO2H

Molecular formula: C84H121ClN18O17

Fields of Application

Assisted reprodution

Ganirelix is an injectable competitive gonadotropin-releasing hormone antagonist (GnRH antagonist). It is primarily used in assisted reproduction to control ovulation. Ganirelix is used in fertility treatments to prevent premature ovulation that could result in the harvesting of eggs that are too immature to be used in procedures such as in vitro fertilization.

Glucagon

CAS number: 
16941-32-5

Sequence
H-His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-Thr-OH

Molecular formula: C153H225N43O49S

Molecular weight: 3482.75 a.m.u.

Fields of Application
Hypoglycemia

Description
Glucagon improves the synthesis and mobilization of glucose in the liver by controverting the action of insulin. The pancreas releases glucagon when blood sugar (glucose) levels fall too low. Glucagon causes the liver to convert stored glycogen into glucose, which is released into the bloodstream. This is the opposite action of insuline, which allows glucose to be taken up and used by insulin-dependent tissues. Thus, glucagon and insulin are part of a feedback system that keeps blood glucose levels at a stable level.

Administration:
Regular injectable form.

 

Gonadorelin

CAS number: 
33515-09-2 (net)
52699-48-6 (acetate)

Sequence
Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2

Molecular formula: C55H75N17O13

Molecular weight: 1181.6 a.m.u.

Fields of Application
Reproduction.
Diagnosis of hypothalamic-pituitary-gonadal function
Veterinary:  Reproduction
Ovarian cysts

Description

Gonadorelin or gonadotropin-releasing hormone (LHRH, also known as GnRH) is a ten amino acid peptide that is synthesized and secreted from hypothalamic neurons and binds to receptors on gonadotrophs.

Gonadorelin causes the pituitary gland to release other hormones (luteinizing hormone [LH] and follicle-stimulating hormone [FSH]). LH and FSH control development in children and fertility in adults. In both sexes LH stimulates secretion of sex steroids from the gonads. LH binds to receptors on Leydig cells, in the testes stimulating synthesis and secretion of testosterone, and in the ovary stimulating secretion of estrogens.

Gonadorelin is used to test how well the hypothalamus and the pituitary glands are working. It is also used to cause ovulation (release of an egg from the ovary) in women who do not have regular ovulation and menstrual periods because the hypothalamus gland does not release enough LHRH.

Administration:
Regular injectable form.

Goserelin

CAS number: 
65807-02-5 (net)
145781-92-6 (acetate)

Sequence
H-Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHNHCONH2.CH3CO2H

Molecular formula: C61H88N18O16

Molecular weight: 1329.5 a.m.u.

Fields of Application
Decrease of reproductive hormones

Description

Goserelin Acetate is the acetate salt of a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH). Continuous, prolonged administration of goserelin in males results in inhibition of pituitary gonadotropin secretion, leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.

Administration:
Regular injectable form.

i
Icatibant

CAS number:
130308-48-4
138614-30-9 (acetate salt)

Sequence
H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH Acetate salt

Molecular formula: C59H89N19O13S

Molecular weight: 1304.5 a.m.u.

Fields of Application
Treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency

Description
Icatibant is an antagonist of the human bradykinin B2 receptor (B2R), that can be used for the treatment of hereditary angioedema (HAE). Upon administration, icatibant targets and binds to B2R, thereby preventing bradykinin from binding to the B2R. This may prevent bradykinin/B2R-mediated vasodilation, the resulting increase in vascular permeability, and the swelling, inflammation, and pain associated with HAE. This may also prevent or improve pulmonary edema not associated with HAE and improve the associated decrease in blood oxygen levels.

Administration:
Regular injectable form.

l
Lanreotide

CAS number:
108736-35-2

Sequence
cyclo(Cys(2)-Cys(7)) H-D-2-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2

Molecular formula: C54H69N11O10S2

Molecular weight: 1096.3 a.m.u.

Fields of Application
Acromegaly
Neuroendocrine tumors (carcinoid syndrome and VIPomas)
Polycystic liver disease

Description
Lanreotide is a synthetic analogue of somatostatin, a naturally occurring inhibitory hormone which blocks the release of several other hormones, including growth hormone, thyroid-stimulating hormone (TSH), insulin and glucagon. Lanreotide binds to the same receptors as somatostatin, although with higher affinity to peripheral receptors, and has similar activity. However, while somatostatin is quickly broken down in the body, lanreotide has a much longer half-life, and produces far more prolonged effects.

Administration:
Regular injectable form.

Lecilerin

CAS number: 
61012-19-9

Sequence
pGlu-His-Trp-Ser-Tyr-D-t-Leu-Leu-Arg-Pro-NHEt

Molecular formula: C59H84N16O12

Molecular weight: 1209.4 a.m.u.

Fields of Application
Veterinary: Lecirelin is used for the induction of ovulation in cows, mares and rabbits and for the treatment of cystic ovarian acyclia in cows.

Description
Lecirelin is a synthetic polypeptide which acts as LH-RH (Luteinizing-hormone releasing hormone) analogue agonist. LH-RH is secreted in the hypothalamus and its release induces the secretion of LH (Luitenizing hormone) and FSH (Follicle-stimulating hormone) from the pituitary gland. These two hormones act on the ovaries and the testes and are responsible of the profertility effects of LHRH through the release of steroideal hormones.

Administration:
Regular injectable form.

Leuprolide

CAS number: 
53714-56-0 (net)
74381-53-6 (acetate)

Sequence
Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NH-CH2-CH3

Molecular formula: C59H84N16O12

Molecular weight: 1209.42 a.m.u.

Fields of Application
Prostate Cancer and breast Cancer
Endometriosis and central precocious puberty

Description
Leuprolide is a synthetic polypeptide which acts as LH-RH (Luteinizing-hormone releasing hormone) analogue agonist. LH-RH is secreted in the hypothalamus and its release induces the secretion of LH (Luitenizing hormone) and FSH (Follicle-stimulating hormone) from the pituitary gland. These two hormones act on the ovaries and the testes and are responsible of the profertility effects of LHRH through the release of steroideal hormones. It is used to treat a number of medical problems, which include: anaemia caused by bleeding of uterine leiomyomas (tumours in the uterus), cancer of the prostate gland in men, central precocious puberty (CPP) and pain due to endometriosis in women.

When given regularly to men and boys, leuprolide decreases testosterone levels. When given regularly to women and girls, leuprolide decreases estrogens levels. By shrinking tumours in the uterus, leuprolide helps stop anaemia by decreasing the vaginal bleeding from these tumours. Iron supplements should be used to help treat the anaemia.

When given to boys and girls experiencing early puberty, leuprolide slows down the development of the genital areas in both sexes and breast development in girls. This medicine delays puberty in a child only as long as the child continues to receive it.

Suppressing estrogens can also cause thinning of the bones or slowing of their growth. This is a positive effect in girls and boys whose bones grow too fast when puberty begins too early.

Administration:
Regular injectable form and Depot injectable form.

Linaclotide

CAS number: 
851199-59-2

Sequence
H-Cys(1)-Cys(2)-Glu-Tyr-Cys(3)-Cys(1)-Asn-Pro-Ala-Cys(2)-Thr-Gly-Cys(3)-Tyr-OH

Molecular formula: C59H79N15O21S6

Molecular weight: 1526.8 a.m.u.

Fields of Application
Treatment of irritable bowel syndrome (IBS) with constipation and chronic idiopathic constipation

Description:

Linaclotide is an oligo-peptide agonist of guanylate cyclase 2C and remains in the GI tract after it is taken orally. This drug is used to treat irritable bowel syndrome with constipation and chronic constipation with no known cause.

Administration:

Oral

n
Nesiritide

CAS number: 
124584-08-3

Sequence
H-Ser-Pro-Lys-Met-Val-Gln-Gly-Ser-Gly-Cys(1)-Phe-Gly-Arg-Lys-Met-Asp-Arg-Ile-Ser-Ser-Ser-Ser-Gly-Leu-Gly-Cys(1)-Lys-Val-Leu-Arg-Arg-His-OH

Molecular formula: C143H244N50O42S4

Molecular weight: 3464.1 a.m.u.

Fields of Application
Smooth muscle cell relaxation

Description:

Nesiritide is the recombinant form of the 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium. Nesiritide works to facilitate cardiovascular fluid homeostasis through counterregulation of the renin–angiotensin–aldosterone system, stimulating cyclic guanosine monophosphate, leading to smooth muscle cell relaxation.

Administration:

Intravenous injection.

o
Octreotide

CAS number: 
83150-76-9 (net)
79517-01-4 (acetate)

Sequence
Cyclo(2-7)D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Throl

Molecular formula: C49H66N10O10S2

Molecular weight: 1019.3 a.m.u.

Fields of Application
Acromegaly
Carcinoid Syndrome
Gastrointestinal haemorrhage

Description
Octreotide is a Somatostatin analogue which has increased biodisponibility due to the presence of a residue of D-Phe at the N-terminus and a residue of threoninol at the C-terminus which makes it more resistant to body enzymes. Since its discovery in 1980 it has proved to inhibit Growth Hormone and inhibit also in part glucagon and insulin. However, this peptide is quite selective in inhibiting the secretion of GH without affecting severely the levels of insulin and glucagon in blood.

Octreotide is used to treat the severe diarrhoea and other symptoms that occur with certain intestinal tumours.

It is also used to treat a condition called acromegaly, which is caused by excessive levels of growth hormone in the body. Octreotide works by reducing the amount of growth hormone that the body produces.

Administration:
Regular injectable form and Depot injectable form.

p
Pasireotide

CAS number:
396091-73-9

Sequence
Cyclo(Phg-D-Trp-Lys-Tyr(Bzl)-Phe-Hyp(2-aminoethyl-carbamoyl))

Molecular formula: C58H66N10O9

Molecular weight: 1047.2 a.m.u.

Fields of Application
Acromegaly
Cushing’s disease

Description
Pasireotide is a synthetic peptide analogue of somatostatin that resembles the native hormone in its ability to suppress levels and activity of growth hormone, insulin, glucagon and many other gastrointestinal peptides. Because its half-life is longer than somatostatin, pasireotide can be used clinically to treat neuroendocrine pituitary tumors that secrete excessive amounts of growth hormone causing acromegaly, or adrenocorticotropic hormone (ACTH) causing Cushing disease.

Administration:
Regular injectable form.

Pramlintide

CAS number:
151126-32-8

Sequence
H-Lys-Cys(1)-Asn-Thr-Ala-Thr-Cys(1)-Ala-Thr-Gln-Arg-Leu-Ala-Asn-Phe-Leu-Val-His-Ser-Ser-Asn-Asn-Phe-Gly-Pro-Ile-Leu-Pro-Pro-Thr-Asn-Val-Gly-Ser-Asn-Thr-Tyr-NH2

Molecular formula: C171H267N51O53S2

Molecular weight: 3949.4 a.m.u.

Fields of Application
Regulation of glucose homeostasis
Diabetes (type 1 and 2)

 

Description
Pramlintide is a peptide analogue of human amylin with 3 proline substitutions at positions 25, 28 and 29, with antihyperglycemic activity. By mimicking amylin, pramlintide slows gastric emptying, inhibits digestive secretions (gastric acid, pancreatic enzymes, and bile), reduces glucagon secretion, and increases satiety; all of these actions are mediated mostly by glucose-sensitive areas in the brain stem. The overall result is a decrease in blood glucose levels.

Administration:
Regular injectable form.

Protirelin

CAS number: 
24305-27-9

Sequence
Pyr-His-Pro-NH2

Molecular formula: C16H22N6O4

Molecular weight: 362.4 a.m.u.

Fields of Application
Diagnosis of Pituitary and Thyroid function

Description
Protirelin is also Known as Thyroptropin-releasing Hormone (TRH). TRH stimulates thyroid-stimulating hormone (TSH) secretion from the anterior pituitary. TSH then initiates thyroid hormone (TH) synthesis and release from the thyroid gland.

The concentration of thyroid hormones in the circulation is regulated by an homeostatic feedback loop involving the hypothalamo-pituitary axis. The main effect of thyroid hormones is to reduce the response of the pituitary thyrotrophs to TRH rather than altering the secretion rate of TRH from the hypothalamus. The sensitivity of the thyrotrophs to TRH depends on their intracellular concentration of T3, 80% of which is derived from the intrapituitary conversion of T4 to T3. When circulating concentrations of T4 are low, there is an increase in the number of TRH receptors and in TSH synthesis resulting in an increased TSH response to TRH. The reverse is true in the presence of high circulating concentrations of thyroid hormones. The TSH response to a bolus injection of TRH has been used to diagnose the exact cause of hypo- and hyper-thyroidism.

Administration:
Regular injectable form.

s
Salmon Calcitonin

CAS number: 
47931-85-1

Sequence
Cyclo(1-7)Cys-Ser-Asn-Leu-Ser-Thr-Cys-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Gly-Thr-Pro-NH2

Molecular formula: C145H240N44O48S2

Molecular weight: 3432 a.m.u.

Fields of Application
Osteoporosis
Hypercalcemia
Paget’s disease

Description
Calcitonin (salmon) is a hormone known to participate in calcium and phosphorous metabolism. Calcitonin is a 32 amino acid peptide, cleaved from a larger prohormone. It contains a single disulfide bond.

Calcitonin lowers the calcium concentration in plasma of mammals by diminishing the rate of bone resorption. It prevents the release of calcium and phosphorous into blood by inhibiting the osteoclasts, a cell type that “digests” bone matrix. It is obtained by chemical synthesis and is available in acetate form.

Calcitonins are used to treat severe hypercalcemia of various origins, Paget’s disease, osteoporosis of various origins, and intractable cancer pain in patients with malignant bone metastases.

Administration:
Regular injectable form and Nasal Spray.

Setmelanotide

CAS number:
920014-72-8

Sequence
Ac-Arg-Cys(1)-D-Ala-His-D-Phe-Arg-Trp-Cys(1)-NH2

Molecular formula: C49H68N18O9S2

Molecular weight: 1117.3 a.m.u.

Fields of Application
Obesity

Description
Setmelanotide is indicated for chronic weight management in people six years and older with obesity due to three rare genetic conditions: pro-opiomelanocortin (POMC) deficiency, proprotein subtilisin/kexin type 1 (PCSK1) deficiency, and leptin receptor (LEPR) deficiency confirmed by genetic testing demonstrating variants in POMC, PCSK1, or LEPR genes considered pathogenic, likely pathogenic, or of uncertain significance. Setmelanotide is the first FDA-approved treatment for these genetic conditions.

Administration:
Regular injectable form.

 

Somatostatin

CAS number: 
38916-34-6 (net)
38916-34-6 (acetate)

Sequence
Cyclo(3-14)Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys

Molecular formula: C76H104N18O19S2

Molecular weight: 1638 a.m.u.

Fields of Application
Gastrointestinal haemorrhage, including bleeding from oesophageal varices
Postoperative pancreatic and duodenal fistulae
Treatment of cancer has been also reported

Description
Somatostatin is a hypothalamic release-inhibiting hormone which inhibits the release of the growth hormone from the anterior pituitary. It can also be found in the stomach, thyroid, intestine, salivary glands and in the pancreas.

At the hypothalamic tract, Somatostatin regulates the secretory activity of the cellules of the anterior pituitary. In several animal species it also inhibits the release of GH and TSH without affecting the release of hormones such as FSH and ACTH.

In the Pancreas Somatostatin inhibits the endocrinal (insulin and glucagon) and esocrinal (bicarbonate, water and pancreatic enzymes) secretions, in basal conditions and as well under alimentary stimulus.

The intravenous infusion of 100 µg or more of Somatostatin induces reduced circulating concentrations of growth hormone in patients with acromegaly. It may also inhibit the release of thyrotropin and corticothropin from the pituitary.

Administration:
Regular injectable form.

t
Teduglutide

CAS number:
197922-42-2

Sequence
H-His-Gly-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-Leu-Ala-Ala-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gln-Thr-Lys-Ile-Thr-Asp-OH

Molecular formula: C164H252N44O55S

Molecular weight: 3752.1 a.m.u.

Fields of Application
Short Bowel Syndrome

Description
Teduglutide is a 33-membered polypeptide and glucagon-like peptide-2 (GLP-2) analog that is used for the treatment of short bowel syndrome. It works by promoting mucosal growth and possibly restoring gastric emptying and secretion.

Administration:
Subcutaneous injection.

Teriparatide

CAS number:
52232-67-4 (net)
99294-94-7 (acetate)

Sequence
H2N-Ser-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Asn-Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-Phe-OH

Molecular formula: C181H291N55O51S2

Molecular weight: 4117.8 a.m.u.

Fields of Application
Osteoporosis
Diagnosis of hypoparathyroidism

Description
pTH (1-34) (human) corresponds to N-terminal part of human parathyroid hormone, a peptide consisting of 84 amino acids. pTH (1-34) (human) shows the same activity and pharmacological profile as the native peptide hormone.

Teriparatide is indicated for use in postmenopausal women with osteoporosis at a high risk for fracture or with a history of osteoporotic fracture, patients with multiple risk factors for fracture, and for patients who have failed or are intolerant to other available osteoporosis therapy.

Intermittent administration of pTH (1-34) (human) acetate in low dosage stimulates bone formation and increases bone mineral density.

Administration:
Regular injectable form.

Terlipressin

CAS number: 
14636-12-5

Sequence
Cyclo(4-9)Gly-Gly-Gly-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Lys-Gly-NH2

Molecular formula: C52H74N16O15S2

Molecular weight: 1226.49 a.m.u.

Fields of Application
Bleeding oesophageal varices.
Hepatorenal syndrome.
Refractory hypotension
Skin burns
Septic shock resistance

 

Description
Terlipressin is an inactive prodrug which is slowly converted in the body to Lypressin, and has the general physiological actions of Vasopressin. Vasopressin, also known as Antidiuretic hormone, is a nine amino acid peptide secreted from the posterior pituitary that regulates water reabsorption in the collecting tubules and salt transport.

Administration:
Regular injectable form.

Tetracosactide

CAS number: 
16960-16-0 (net)
60189-34-6 (acetate)

Sequence
H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys- Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-OH

Molecular formula: C136H210N40O31S

Molecular weight: 2933.5 a.m.u.

Fields of Application
Diagnosis of adrenocortical insufficiency
As alternative to systemic corticosteroid therapy

Description
Tetracosactide (cosyntropin) is a synthetic analogue of the naturally-occurring hormone, adrenocorticotrophic hormone (ACTH).

In the normal situation, ACTH is released from the pituitary gland in the brain. It acts on the adrenal glands to stimulate the production of steroid hormones (glucocorticoids and mineralocorticoids), and, to a lesser extent, androgens (male sex hormones). If the adrenal glands are healthy, a single injection of tetracosactide results in a rise in blood cortisol (hydrocortisone) concentrations in 30 minutes.

If the adrenal glands appear not to be working then tetracosactide injection can be given to check whether the problem is due to diseased or damaged adrenals or due to lack of pituitary ACTH.

Tetracosacatide has also been used therapeutically for most of the conditions in which systemic corticosteroid therapy is indicated.

For diagnostic purposes tetracosactide acetate is used intramuscularly or intravenously as a plain injection in the first instance, then, if results are inconclusive, intramuscularly as a long-acting depot injection.

Administration:
Regular injectable form and Depot injectable form.

Thymosin A1

CAS number: 
62304-98-7

Sequence
As-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn-OH

Molecular formula: C129H215N33O55

Molecular weight: 3108.3 a.m.u.

Fields of Application
Hepatitis B and C

 

Description
The thymus gland controls the development of T-lymphocytes and thereby plays a central role in cell-mediated immunity and in the regulation of immune responses. Several polypeptides characterised in the thymus or serum are able to induce lymphocyte differentiation in vitro and in vivo.

Thymosin A1, also known as Thymalfasin is used alone or in combination with interferon as an immunomodulator for the treatment of chronic hepatitis B and C. It is also used to enhance the effectiveness of influenza vaccines in immunocompromised or elderly patients and of influenza and hepatitis B vaccines in chronic haemodialysis patients.

Thymosin A1 is under investigation for a number of other diseases, including hepatitis D, hepatocellular carcinoma, non-small cell lung cancer, melanoma, and HIV infection and AIDS.

Administration:
Regular injectable form.

Triptorelin

CAS number: 
57773-63-4 (net)
140194-24-7 (acetate)

Sequence
Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2

Molecular formula: C64H82N18O13

Molecular weight: 1311.47 a.m.u.

Fields of Application
Reproduction
Prostate Cancer
Endometriosis
Precocious central puberty

Description
Triptorelin is a luteinizing hormone-releasing hormone (LHRH) agonist. The only change between LHRH and Triptorelin is the introduction of a residue of D-Triptophane instead of a glycine in position 6. The vast majority of LHRH analogue agonists show changes in this position.

The subcutaneous and/or intramuscular injection of Triptorelin in solution or by means of depot formulations containing the peptide has shown efficacy in the treatment of ovarian carcinoma, prostatic carcinoma, endometriosis, uterine leiomyoma, fibrocystic breast disease, and precocious puberty; its use has been beneficial during in vitro fertilization protocols.

The product controls release of Luteinizing Hormone (LH) and Follicle Stimulating Hormone (FSH) and also levels of testoterone and estrogen. When given regularly to men, triptorelin decreases testosterone levels. Reducing the amount of testosterone in the body is one way of treating cancer of the prostate.

Administration:
Regular injectable form and Depot injectable form.

v
Vasoactive Intestinal Peptide

CAS number: 
40077-57-4

Sequence
H-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Leu-Asn-NH2

Molecular formula: C147H238N44O42S

Molecular weight: 3325.9 a.m.u.

Fields of Application
Treatment of primary pulmonary hypertension
Erectile dysfunction

 

Description
Vasoactive intestinal peptide acts as a hormone and neurotransmitter in various parts of the body; it is a potent relaxant of smooth muscle and has vasodilator and bronchodilator properties as well as stimulating the gastrointestinal tract to increased secretion. It has been tried for many different biological actions and more recently for the treatment of erectile dysfunction.

Administration:
Inhalation.

Vosoritide

CAS number: 
1480724-61-5

Sequence
H-Pro-Gly-Gln-Glu-His-Pro-Asn-Ala-Arg-Lys-Tyr-Lys-Gly-Ala-Asn-Lys-Lys-Gly-Leu-Ser-Lys-Gly-Cys(1)-Phe-Gly-Leu-Lys-Leu-Asp-Arg-Ile-Gly-Ser-Met-Ser-Gly-Leu-Gly-Cys(1)-OH

Molecular formula: C176H290N56O51S3

Molecular weight: 4102.8 a.m.u.

Fields of Application
Achondroplasia

Description
Achondroplasia is an autosomal dominant genetic disease and the most common cause of dwarfism in humans. It results from a gain-of-function missense mutation in FGFR3 that results in a dramatic suppression of bone growth, both in volume and in length.

Endogenous CNP, first described in 1998, is primarily responsible for the stimulation of chondrocytes and long bone growth via activity at the NPR-B receptor, where Vosoritide is an analog of CNP with proline-glycine on its N-terminus to convey resistance to neutral endopeptidase.

 

Administration:
Subcutaneous injection

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