Triptorelin Pamoate

Triptorelin pamoate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.

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CAT#	10-101-101
CAS	57773-63-4 (net), 124508-66-3 (pamoate salt)
Background	Triptorelin Pamoate (also called Triptorelin Embonate) is a potent LHRH (GnRH) agonist. Triptorelin Pamoate is a salt form of triptorelin suitable for obtaining controlled release formulations. After a transient increase, continuous administration of triptorelin results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
Synonyms/Alias	5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-prolylglycine amide, 4,4'-methylenebis(3-hydroxy-2-naphthoate) (salt); Decapeptyl; Diphereline; Gonapeptyl; Luteinizing hormone-releasing factor (swine), 6-D-tryptophan-, 4,4'-methylenebis(3-hydroxy-2-naphthalenecarboxylate) (salt); Pamorelin; Trelstar; Trelstar depot; Trelstar LA; Triptorelin embonate; UNII-08AN7WA2G0
M.F/Formula	C64H82N18O13
M.W/Mr.	1744.96
Sequence	Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
Labeling Target	Gonadotropin-releasing hormone (GNRH) Receptor
Application	Triptorelin pamoate is classified as a gonadotropin releasing hormone (GnRH) agonist. In adult men with advanced prostate cancer, triptorelin pamoate can be used to help lower testosterone levels, which can be beneficial in stopping or slowing the growth of abnormal prostate tissue.
Activity	Agonist
Biological Activity	Triptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts.
Areas of Interest	Cancer Research Pituitary & Hypothalamic Hormones Veterinary Medicine
Functions	Peptide binding
Target	Gonadotropin-releasing hormone (GnRH)

CAT#	Product Name	M.W	Molecular Formula	Inquiry
10-101-01	Tetracosactide Acetate	2933.5	C136H210N40O31S	Inquiry
10-101-31	Sincalide Ammonium Salt	1143.3	C49H62N10O16S3	Inquiry
10-101-32	Somatostatin Acetate	1637.88		Inquiry
10-101-41	Splenopentin Acetate	813.89	C35H59N9O13	Inquiry
10-101-63	Taltirelin	477.46	C17H23N7O5	Inquiry

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Source#	Synthetic
Long-term Storage Conditions	−20°C
Organism	Human
References	Gonadotropin-releasing hormone agonists are widely used as androgen deprivation therapy in many men with locally advanced or metastatic prostate cancer. Gonadotropin-releasing hormone agonists are delivered by intramuscular injection every 1, 3 or 6 months, but in some patients subcutaneous injection may be more appropriate. This study assessed the efficacy and safety profile of the gonadotropin-releasing hormone agonist, triptorelin pamoate, when administered by the subcutaneous route. Lebret, T., Rouanne, M., Hublarov, O., Jinga, V., Petkova, L., Kotsev, R., ... & Dutailly, P. (2015). Efficacy of triptorelin pamoate 11.25 mg administered subcutaneously for achieving medical castration levels of testosterone in patients with locally advanced or metastatic prostate cancer. Therapeutic advances in urology, 7(3), 125-134. To compare the efficacy of monthly administrations of the luteinizing hormone-releasing hormone agonists triptorelin pamoate and leuprolide acetate to induce and maintain castrate levels of serum testosterone in men with advanced prostate cancer. Triptorelin reduced testosterone concentrations less rapidly, but maintained castration as effectively as leuprolide. There was no evidence that the slower onset of castration caused deleterious effects. Heyns, C. F., Simonin, M. P., Grosgurin, P., Schall, R., & Porchet, H. C. (2003). Comparative efficacy of triptorelin pamoate and leuprolide acetate in men with advanced prostate cancer. BJU international, 92(3), 226-231.