LKT Labs

Biochemicals for Life Science Research

Histrelin Acetate

Product ID H3277
Cas No. 76712-82-8
Purity ≥95%
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Description

Histrelin is an anti-estrogen, anti-testosterone analog of gonadotropin-releasing hormone (GnRH) or luteinizing hormone releasing hormone (LHRH). Histrelin binds and activates the GnRH/LHRH receptor, initially stimulating release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), but then inducing desensitization and decreasing levels of these hormones over long-term administration. Histrelin is clinically used to treat precocious puberty and to suppress estrogen and testosterone levels in prostate cancer patients.

Product Info

Cas No.

76712-82-8
Purity

≥95%
Formula

C66H86N18O12
Formula Wt.

1323.52
IUPAC Name

(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-3-(1-benzylimidazol-4-yl)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Synonym

[des-Gly 10, D-His(Bzl) 6]-LH-RH ethylamide
Solubility

Soluble in DMSO.

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

H3277 MSDS PDF
Info Sheet

H3277 Info Sheet PDF

References

Lewis KA, Goldyn AK, West KW, et al. A single histrelin implant is effective for 2 years for treatment of central precocious puberty. J Pediatr. 2013 Oct;163(4):1214-6. PMID: 23809043.

Shore N, Cookson MS, Gittelman MC. Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU Int. 2012 Jan;109(2):226-32. PMID: 21851539.

Barradell LB, McTavish D. Histrelin. A review of its pharmacological properties and therapeutic role in central precocious puberty. Drugs. 1993 Apr;45(4):570-88. PMID: 7684676.

Gunnet JW, Demarest KT, Hahn DW, et al. Effects of a sustained release formulation of the gonadotrophin-releasing hormone agonist histrelin on serum concentrations of gonadotrophins and oestradiol, and ovarian LH/human chorionic gonadotrophin receptor content in the rat. J Endocrinol. 1991 Nov;131(2):211-8. PMID: 1744568.

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