Buserelin Acetate | CAS#68630-75-1 | GnRH agonist

MedKoo Cat#: 562478 | Name: Buserelin Acetate

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Buserelin Acetate is a Gonadotropin-releasing hormone agonist (GnRH agonist).

Chemical Structure

Buserelin Acetate

CAS#68630-75-1 (acetate)

Theoretical Analysis

MedKoo Cat#: 562478

Name: Buserelin Acetate

CAS#: 68630-75-1 (acetate)

Chemical Formula: C62H90N16O15

Exact Mass: 1298.6772

Molecular Weight: 1299.49

Elemental Analysis: C, 57.31; H, 6.98; N, 17.25; O, 18.47

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 350.00	2 Weeks

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Related CAS #

68630-75-1 (free base) 68630-75-1 (acetate)

Synonym

HOE-766; HOE 766; HOE766; Buserelin Acetate;

IUPAC/Chemical Name

5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate

InChi Key

PYMDEDHDQYLBRT-DRIHCAFSSA-N

InChi Code

InChI=1S/C60H86N16O13.C2H4O2/c1-7-64-57(87)48-15-11-23-76(48)58(88)41(14-10-22-65-59(61)62)69-51(81)42(24-33(2)3)70-56(86)47(31-89-60(4,5)6)75-52(82)43(25-34-16-18-37(78)19-17-34)71-55(85)46(30-77)74-53(83)44(26-35-28-66-39-13-9-8-12-38(35)39)72-54(84)45(27-36-29-63-32-67-36)73-50(80)40-20-21-49(79)68-40;1-2(3)4/h8-9,12-13,16-19,28-29,32-33,40-48,66,77-78H,7,10-11,14-15,20-27,30-31H2,1-6H3,(H,63,67)(H,64,87)(H,68,79)(H,69,81)(H,70,86)(H,71,85)(H,72,84)(H,73,80)(H,74,83)(H,75,82)(H4,61,62,65);1H3,(H,3,4)/t40-,41-,42-,43-,44-,45-,46-,47+,48-;/m0./s1

SMILES Code

O=C(NCC)[C@H]1N(C([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@@H](COC(C)(C)C)NC([C@H](CC2=CC=C(O)C=C2)NC([C@H](CO)NC([C@H](CC3=CNC4=C3C=CC=C4)NC([C@H](CC5=CNC=N5)NC([C@H](CC6)NC6=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1.CC(O)=O

Appearance

Solid powder

Purity

>98% (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

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

TBD

In vitro activity:

Representative current traces obtained in non-treated and buserelin treated CF HNEC are shown in Fig 3A. This study showed that the amplitudes of the currents were higher in the presence of buserelin and that buserelin permits CFTR to respond to its specific activators and inhibitor. Reference: PLoS One. 2017; 12(11): e0187774. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5690610/

In vivo activity:

After in vivo buserelin treatment in rats, the frequency of splenic Tregs was decreased, with the reduction in the expression of Foxp3, IL-10, and TGF-β. The suppressive activity of Tregs was weakened. Reference: Acta Cir Bras. 2017 Feb;32(2):140-147. https://pubmed.ncbi.nlm.nih.gov/33586576/

Preparing Stock Solutions

The following data is based on the product molecular weight 1,299.49 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.

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:

1. Li H, Zhu XX, Xiang JB, Jian L. Buserelin Inhibits the Immunosuppressive Activity of Regulatory T Cells through the Protein Kinase A Signaling in a Central Precocious Puberty Model. Immunol Invest. 2021 Feb 15:1-15. doi: 10.1080/08820139.2021.1885437. Epub ahead of print. PMID: 33586576. 2. Calvez ML, Benz N, Huguet F, Saint-Pierre A, Rouillé E, Coraux C, Férec C, Kerbiriou M, Trouvé P. Buserelin alleviates chloride transport defect in human cystic fibrosis nasal epithelial cells. PLoS One. 2017 Nov 16;12(11):e0187774. doi: 10.1371/journal.pone.0187774. PMID: 29145426; PMCID: PMC5690610. 3. Khadivi B, Peirouvi T, JavanmardI MZ, Rasmi Y. Short-term buserelin administration induces apoptosis and morphological changes in adult rat testes. Acta Cir Bras. 2017 Feb;32(2):140-147. doi: 10.1590/s0102-865020170206. PMID: 28300875.

In vitro protocol:

In vivo protocol:

1: Trasorras VL, Carretero MI, Neild DM, Chaves MG, Giuliano SM, Miragaya MH. Production, Preservation, and Transfer of South American Camelid Embryos. Front Vet Sci. 2017 Nov 13;4:190. doi: 10.3389/fvets.2017.00190. eCollection 2017. Review. PubMed PMID: 29181380; PubMed Central PMCID: PMC5693846. 2: Kasum M, Orešković S, Franulić D, Čehić E, Lila A, Vujić G, Grgić F. Current Medical Strategies in the Prevention of Ovarian Hyperstimulation Syndrome. Acta Clin Croat. 2017 Mar;56(1):133-142. doi: 10.20471/acc.2017.56.01.19. Review. PubMed PMID: 29120551. 3: Ohlsson B. Gonadotropin-Releasing Hormone and Its Role in the Enteric Nervous System. Front Endocrinol (Lausanne). 2017 Jun 7;8:110. doi: 10.3389/fendo.2017.00110. eCollection 2017. Review. PubMed PMID: 28638366; PubMed Central PMCID: PMC5461264. 4: Bale S, Khurana A, Reddy AS, Singh M, Godugu C. Overview on Therapeutic Applications of Microparticulate Drug Delivery Systems. Crit Rev Ther Drug Carrier Syst. 2016;33(4):309-361. Review. PubMed PMID: 27910739. 5: Ohlsson B. Gonadotropin-Releasing Hormone and Its Physiological and Pathophysiological Roles in Relation to the Structure and Function of the Gastrointestinal Tract. Eur Surg Res. 2016;57(1-2):22-33. doi: 10.1159/000445717. Epub 2016 Apr 19. Review. PubMed PMID: 27089503. 6: Siristatidis CS, Gibreel A, Basios G, Maheshwari A, Bhattacharya S. Gonadotrophin-releasing hormone agonist protocols for pituitary suppression in assisted reproduction. Cochrane Database Syst Rev. 2015 Nov 9;(11):CD006919. doi: 10.1002/14651858.CD006919.pub4. Review. PubMed PMID: 26558801. 7: Andres Mde P, Lopes LA, Baracat EC, Podgaec S. Dienogest in the treatment of endometriosis: systematic review. Arch Gynecol Obstet. 2015 Sep;292(3):523-9. doi: 10.1007/s00404-015-3681-6. Epub 2015 Mar 8. Review. PubMed PMID: 25749349. 8: Brown J, Farquhar C. An overview of treatments for endometriosis. JAMA. 2015 Jan 20;313(3):296-7. doi: 10.1001/jama.2014.17119. Review. PubMed PMID: 25603001. 9: Abacı A, Çatlı G, Anık A, Böber E. Epidemiology, classification and management of undescended testes: does medication have value in its treatment? J Clin Res Pediatr Endocrinol. 2013;5(2):65-72. doi: 10.4274/Jcrpe.883. Review. PubMed PMID: 23748056; PubMed Central PMCID: PMC3701924. 10: Gerlinger C, Faustmann T, Hassall JJ, Seitz C. Treatment of endometriosis in different ethnic populations: a meta-analysis of two clinical trials. BMC Womens Health. 2012 Apr 19;12:9. doi: 10.1186/1472-6874-12-9. Review. PubMed PMID: 22515510; PubMed Central PMCID: PMC3470994. 11: Pinto E, Pinelo S, Osório M, Ferreira C, Serra H, Pires I, Barbosa A, Figueiredo H, Felgueira E, Tavares A. Outcomes from ovarian hyperstimulation following the sole administration of gonadotrophin-releasing hormone agonist in the context of in vitro fertilization: report of two cases and review of the literature. Gynecol Endocrinol. 2012 Jul;28(7):545-8. doi: 10.3109/09513590.2011.650745. Epub 2012 Mar 23. Review. PubMed PMID: 22439899. 12: Humaidan P, Papanikolaou EG, Kyrou D, Alsbjerg B, Polyzos NP, Devroey P, Fatemi HM. The luteal phase after GnRH-agonist triggering of ovulation: present and future perspectives. Reprod Biomed Online. 2012 Feb;24(2):134-41. doi: 10.1016/j.rbmo.2011.11.001. Epub 2011 Nov 9. Review. PubMed PMID: 22197130. 13: Maheshwari A, Gibreel A, Siristatidis CS, Bhattacharya S. Gonadotrophin-releasing hormone agonist protocols for pituitary suppression in assisted reproduction. Cochrane Database Syst Rev. 2011 Aug 10;(8):CD006919. doi: 10.1002/14651858.CD006919.pub3. Review. Update in: Cochrane Database Syst Rev. 2015;11:CD006919. PubMed PMID: 21833958. 14: McCormack PL. Dienogest: a review of its use in the treatment of endometriosis. Drugs. 2010 Nov 12;70(16):2073-88. doi: 10.2165/11206320-000000000-00000. Review. PubMed PMID: 20964453. 15: Kirby RS, Fitzpatrick JM, Clarke N. Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. Review. PubMed PMID: 20053189. 16: Harada T, Taniguchi F. Dienogest: a new therapeutic agent for the treatment of endometriosis. Womens Health (Lond). 2010 Jan;6(1):27-35. doi: 10.2217/whe.09.72. Review. PubMed PMID: 20001868. 17: Novara G, Galfano A, Secco S, Ficarra V, Artibani W. Impact of surgical and medical castration on serum testosterone level in prostate cancer patients. Urol Int. 2009;82(3):249-55. doi: 10.1159/000209352. Epub 2009 May 11. Review. PubMed PMID: 19440008. 18: Kutzler MA. Estrus induction and synchronization in canids and felids. Theriogenology. 2007 Aug;68(3):354-74. Epub 2007 Jun 19. Review. PubMed PMID: 17582484. 19: Tanaka T. [Precocious puberty]. Nihon Rinsho. 2006 Apr;64 Suppl 4:96-100. Review. Japanese. PubMed PMID: 16689292. 20: Taguchi T, Noguchi S. [Clinical applications of GnRHa in breast cancer]. Nihon Rinsho. 2006 Apr;64 Suppl 4:85-9. Review. Japanese. PubMed PMID: 16689290.