Triptorelin pamoate
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MedKoo CAT#: 100894

CAS#: 124508-66-3 (pamoate)

Description: 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. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. It is also used as therapy for gender identity disorder.

Chemical Structure

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Triptorelin pamoate
CAS# 124508-66-3 (pamoate)
Instruction

Theoretical Analysis

MedKoo Cat#: 100894
Name: Triptorelin pamoate
CAS#: 124508-66-3 (pamoate)
Chemical Formula: C87H98N18O19
Exact Mass: 0.00
Molecular Weight: 1,699.850
Elemental Analysis: C, 61.47; H, 5.81; N, 14.83; O, 17.88

Price and Availability

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5mg USD 285 2 Weeks
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Related CAS #: 140194-24-7 (acetate)   57773-63-4 (free base)   124508-66-3 (pamoate)   2240176-35-4 (TFA)    

Synonym: AY25650; AY-25650; AY 25650; CL118532; CL-118532; CL 118532; Wy42462; Wy-42462; Wy4 2462; D-Trp-6-LH-RH; Triptorelin. US brand name: Trelstar Depot. Decapeptyl; Decapeptyl Depot; Decapeptyl LP; Decapeptyl Trimestral; Embonate.

IUPAC/Chemical Name: (S)-1-((3S,6S,9S,12S,15R,18S,21S)-3-((1H-imidazol-5-yl)methyl)-6,15-bis((1H-indol-3-yl)methyl)-21-(3-((diaminomethylene)amino)propyl)-12-(4-hydroxybenzyl)-9-(hydroxymethyl)-18-isobutyl-1,4,7,10,13,16,19-heptaoxo-1-((S)-5-oxopyrrolidin-2-yl)-2,5,8,11,14,17,20-heptaazadocosan-22-oyl)-N-(2-amino-2-oxoethyl)pyrrolidine-2-carboxamide 4,4'-methylenebis(3-hydroxy-2-naphthoate)

InChi Key: ZBVJFYPGLGEMIN-OYLNGHKZSA-N

InChi Code: InChI=1S/C64H82N18O13.C23H16O6/c1-34(2)23-46(56(88)75-45(13-7-21-69-64(66)67)63(95)82-22-8-14-52(82)62(94)72-31-53(65)85)76-58(90)48(25-36-28-70-42-11-5-3-9-40(36)42)78-57(89)47(24-35-15-17-39(84)18-16-35)77-61(93)51(32-83)81-59(91)49(26-37-29-71-43-12-6-4-10-41(37)43)79-60(92)50(27-38-30-68-33-73-38)80-55(87)44-19-20-54(86)74-44;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/h3-6,9-12,15-18,28-30,33-34,44-52,70-71,83-84H,7-8,13-14,19-27,31-32H2,1-2H3,(H2,65,85)(H,68,73)(H,72,94)(H,74,86)(H,75,88)(H,76,90)(H,77,93)(H,78,89)(H,79,92)(H,80,87)(H,81,91)(H4,66,67,69);1-10,24-25H,11H2,(H,26,27)(H,28,29)/t44-,45-,46-,47-,48+,49-,50-,51-,52-;/m0./s1

SMILES Code: CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](CC2=CNC3=CC=CC=C32)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8.C1=CC=C2C(=C1)C=C(C(=C2CC3=C(C(=CC4=CC=CC=C43)C(=O)O)O)O)C(=O)O

Appearance: Solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Triptorelin (free base) Chemical Formula: C64H82N18O13 Exact Mass: 1310.6309 Molecular Weight: 1311.4730 Elemental Analysis: C, 58.61; H, 6.30; N, 19.22; O, 15.86 CAS# related to Triptorelin Triptorelin free base: CAS#57773-63-4 Triptorelin acetate: CAS#140194-24-7 Triptorelin pamoate: CAS#124508-66-3

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,699.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Abbara A, Phylactou M, Eng PC, Clarke SA, Pham TD, M H T, Ng KY, Mills EG, Purugganan K, Hunjan T, Salim R, Comninos AN, Vuong LN, Dhillo WS. Endocrine responses to triptorelin in healthy women, women with Polycystic Ovary Syndrome and Hypothalamic Amenorrhea. J Clin Endocrinol Metab. 2023 Jan 19:dgad026. doi: 10.1210/clinem/dgad026. Epub ahead of print. PMID: 36653328.


2: Zhou Y, Jia R, Kong FS, Chen M, Ren F, Xu Z, Ma Y. A single blood sample for stimulated LH assayed by ICMA is useful for monitoring the treatment efficacy of triptorelin depot in girls. Scand J Clin Lab Invest. 2022 Nov- Dec;82(7-8):588-594. doi: 10.1080/00365513.2022.2148120. Epub 2022 Nov 24. PMID: 36421059.


3: García García E, Álvarez Del Vayo C, Castaño L. Familial male-limited precocious puberty (testotoxicosis): Usefulness of treatment with ketoconazole and triptorelin. Med Clin (Barc). 2022 Dec 9;159(11):e79-e80. English, Spanish. doi: 10.1016/j.medcli.2022.08.007. Epub 2022 Aug 29. PMID: 36049976.


4: Li X, Li H, Shi H, Li X, Zhou R, Lu D, Cai Y, Zhou Y, Cabri P, Shi X, Pedret- Dunn A, Leng J. Assessment of Two Formulations of Triptorelin in Chinese Patients with Endometriosis: A Phase 3, Randomized Controlled Trial. Adv Ther. 2022 Oct;39(10):4663-4677. doi: 10.1007/s12325-022-02264-5. Epub 2022 Aug 10. PMID: 35947347; PMCID: PMC9464738.


5: Uzonwanne VO, Navabi A, Obayemi JD, Hu J, Salifu AA, Ghahremani S, Ndahiro N, Rahbar N, Soboyejo W. Triptorelin-functionalized PEG-coated biosynthesized gold nanoparticles: Effects of receptor-ligand interactions on adhesion to triple negative breast cancer cells. Biomater Adv. 2022 May;136:212801. doi: 10.1016/j.bioadv.2022.212801. Epub 2022 Apr 12. PMID: 35929297.


6: Metbulut AP, Adıgüzel KT, İslamoğlu C, Boyraz M, Mısırlıoğlu ED. Evaluation of Hypersensitivity Reactions with Leuprolide Acetate and Triptorelin Acetate in Children. Indian J Endocrinol Metab. 2021 Nov-Dec;25(6):527-531. doi: 10.4103/ijem.ijem_333_21. Epub 2022 Feb 17. PMID: 35355908; PMCID: PMC8959209.


7: Zhu L, Guan Z, Huang Y, Hua K, Ma L, Zhang J, Yang D, Perrot V, Li H, Zhang X. The efficacy and safety of triptorelin-therapy following conservative surgery for deep infiltrating endometriosis: A multicenter, prospective, non- interventional study in China. Medicine (Baltimore). 2022 Feb 4;101(5):e28766. doi: 10.1097/MD.0000000000028766. PMID: 35119037; PMCID: PMC8812645.


8: Nikzad F, Sadjadi SA, Mohammadpour AH, Ziaee M, Behdani F, Naghibi SM, Nejatifard SN, Ghanbari M, Akhondpour Manteghi A. Adjunct Triptorelin in the Treatment of Obsessive-Compulsive Disorder in Clients Receiving Selective Serotonin Reuptake Inhibitors (SSRIs). Iran J Psychiatry. 2021 Oct;16(4):444-450. doi: 10.18502/ijps.v16i4.7232. PMID: 35082857; PMCID: PMC8725189.


9: Lu X, Sun Y, Han M, Chen D, Wang A, Sun K. Silk fibroin double-layer microneedles for the encapsulation and controlled release of triptorelin. Int J Pharm. 2022 Feb 5;613:121433. doi: 10.1016/j.ijpharm.2021.121433. Epub 2021 Dec 28. PMID: 34968682.


10: Vukovic R, Milenkovic T, Soldatovic I, Pekic S, Mitrovic K, Todorovic S. Triptorelin stimulated luteinizing hormone concentrations for diagnosing central precocious puberty: study of diagnostic accuracy. Endocrine. 2022 Mar;75(3):934-941. doi: 10.1007/s12020-021-02947-z. Epub 2021 Nov 26. PMID: 34826116; PMCID: PMC8616750.


11: Wang L, Jiang Q, Wang M, Xu J, Jin J. The effect of triptorelin and leuprolide on the level of sex hormones in girls with central precocious puberty and its clinical efficacy analysis. Transl Pediatr. 2021 Sep;10(9):2307-2312. doi: 10.21037/tp-21-352. PMID: 34733671; PMCID: PMC8506057.


12: Piešťanský J, Čižmárová I, Štefánik O, Matušková M, Horniaková A, Majerová P, Mikuš P. Capillary Electrophoresis-Mass Spectrometry with Multisegment Injection and In-Capillary Preconcentration for High-Throughput and Sensitive Determination of Therapeutic Decapeptide Triptorelin in Pharmaceutical and Biological Matrices. Biomedicines. 2021 Oct 16;9(10):1488. doi: 10.3390/biomedicines9101488. PMID: 34680605; PMCID: PMC8533539.


13: Chung LY, Kang E, Nam HK, Rhie YJ, Lee KH. Efficacy of Triptorelin 3-Month Depot Compared to 1-Month Depot for the Treatment of Korean Girls with Central Precocious Puberty in Single Tertiary Center. J Korean Med Sci. 2021 Aug 30;36(34):e219. doi: 10.3346/jkms.2021.36.e219. PMID: 34463062; PMCID: PMC8405405.


14: Sun W, Hua K, Hong L, Zhang J, Hao M, Wang J, Zhang J, Perrot V, Li H, Zhang X. Symptom control after different duration of triptorelin treatment following conservative surgery for deep infiltrating endometriosis: Post-hoc analysis of a multicentre, prospective, real-world study. Medicine (Baltimore). 2021 Jul 30;100(30):e26753. doi: 10.1097/MD.0000000000026753. PMID: 34397719; PMCID: PMC8322541.


15: Forsback AP, Noppari P, Viljanen J, Mikkola J, Jokinen M, Leino L, Bjerregaard S, Borglin C, Halliday J. Sustained In-Vivo Release of Triptorelin Acetate from a Biodegradable Silica Depot: Comparison to Pamorelin® LA. Nanomaterials (Basel). 2021 Jun 16;11(6):1578. doi: 10.3390/nano11061578. PMID: 34208450; PMCID: PMC8233906.


16: Yousefvand M, Mohammadi Z, Ghorbani F, Irajirad R, Abedi H, Seyedi S, Papi A, Montazerabadi A. Investigation of Specific Targeting of Triptorelin- Conjugated Dextran-Coated Magnetite Nanoparticles as a Targeted Probe in GnRH+ Cancer Cells in MRI. Contrast Media Mol Imaging. 2021 May 17;2021:5534848. doi: 10.1155/2021/5534848. PMID: 34104122; PMCID: PMC8149228.


17: Aka S, Abali S, Taskin A, Bengur FB, Semiz S. Comparison of two different GnRH analogs' impact on final height in girls with early puberty: Triptorelin acetate vs. leuprolide acetate. Acta Endocrinol (Buchar). 2020 Oct- Dec;16(4):402-408. doi: 10.4183/aeb.2020.402. PMID: 34084230; PMCID: PMC8126396.


18: Martinerie L, de Mouzon J, Blumberg J, di Nicola L, Maisonobe P, Carel JC; PREFER study group. Fertility of Women Treated during Childhood with Triptorelin (Depot Formulation) for Central Precocious Puberty: The PREFER Study. Horm Res Paediatr. 2020;93(9-10):529-538. doi: 10.1159/000513702. Epub 2021 Mar 26. PMID: 33774631; PMCID: PMC8686727.


19: Abdelzaher WY, Abdel-Hafez SMN, Rofaeil RR, Ali AHSA, Hegazy A, Bahaa HA. The protective effect of fenofibrate, triptorelin, and their combination against premature ovarian failure in rats. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jan;394(1):137-149. doi: 10.1007/s00210-020-01975-2. Epub 2020 Sep 14. PMID: 32924068.


20: Andreeva E, Absatarova Y. Triptorelin for the treatment of adenomyosis: A multicenter observational study of 465 women in Russia. Int J Gynaecol Obstet. 2020 Dec;151(3):347-354. doi: 10.1002/ijgo.13341. Epub 2020 Sep 19. PMID: 32815156; PMCID: PMC7756635.