Histrelin acetate 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.
CAT# | 10-101-21 |
CAS | 76712-82-8 (net) |
Background | Histrelin Acetate is the acetate salt form of histrelin, a long-acting, synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) with potential anti-tumor activity. Upon administration, histrelin binds to and activates GnRH receptors; prolonged administration results in pituitary GnRH receptor desensitization and inhibition of follicle stimulating hormone (FSH) and luteinizing hormone (LH) secretion, leading to a significant decline in testosterone production in males and may inhibit androgen receptor-positive tumor progression; in females, prolonged administration results in decreased estradiol production. >> Read More |
Synonyms/Alias | (Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH; L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-L-arginyl-L-proline ethylamide acetic acid |
Chemical Name | acetic acid;(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 |
M.F/Formula | C66H86N18O12 |
M.W/Mr. | 1383.6 |
Sequence | One Letter Code: XHWSYXLRP Three Letter Code: H-Pyr-His-Trp-Ser-Tyr-D-His(1-Bn)-Leu-Arg-Pro-NHEt.CH3CO2H |
Labeling Target | Gonadotropin-releasing hormone receptor |
Application | Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin has been proven to be highly effective in treating central precocious puberty in children. |
Appearance | Solid powder |
Purity | >98% (or refer to the Certificate of Analysis) |
Activity | Agonist |
Areas of Interest | Cardiovascular System & Diseases Pituitary & Hypothalamic Hormones |
Target | Gonadotropin-releasing hormone (GnRH) |
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