| CAS | 220810-26-4 |
| Sequence | Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt |
| Sequence Single | Pyr-HWSYh(Bzl)LRP-NHEt |
| Molecular Formula | C66H86N18O12 |
| Molecular Weight | 1323.52 |
| Synonyms | Histrelin |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Cancer Research|Pituitary & Hypothalamic Hormones |
| Description | (Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH also called Histrelin, is a potent LHRH agonist. Histrelin stimulates LH and FSH release and inhibits the actions of sex steroids on the male and female reproductive tracts. Its potency in vivo and in vitro is similar to that of the D-Trp6-containing analog. Especially because of its high water solubility and greater lipophilic character, histrelin appears promising for clinical application. Slow-release implants containing histreline implants were approved for the palliative treatment of advanced hormone-dependent prostate cancer. CAS Number (histrelin acetate): 76712-82-8. |
| References | 1. Simultaneous separation of hydrophobic and hydrophilic peptides with a silica hydride stationary phase using aqueous normal phase conditions. R.I.Boysen et al., J. Chromatogr. A, 1218, 8021 (2011) 2. Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. N.Shore et al., BJU Int., 109, 226 (2012) 3. 144 ROLE OF GnRH ON MOUSE PRE-IMPLANTATION EMBRYONIC DEVELOPMENT IN VITRO. Merck Index, 15th ed., No. 4760, (2013) 4. Gonadotropin-releasing hormone analog design. Structure-function studies toward the development of agonists and antagonists: rationale and perspective. M.Montagner et al., Reprod. Fertil. Dev., 17, 222 (2004) 5. 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. M.J.Karten and J.E.Rivier, Endocr. Rev., 7, 44 (1986) 6. The effects of the GnRH agonist, [(imBzl)-D-His6, Pro9-NEt]-GnRH, on the response to stress in rats. J.W.Gunnet et al., J. Endocrinol., 131, 211 (1991) 7. Histrelin: in advanced prostate cancer. M.J.Gibson and D.S.Kohtz, Contraception, 31, 91 (1985) 8. Effects of the (imBzl)D-His6, Des-Gly analog of GnRH on gonadotropin and estradiol secretion in normal women. E.D.Deeks, Drugs, 70, 623 (2010) |
(Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH
CAS No.: 220810-26-4
(Des-Gly10,D-His(Bzl)6,Pro-NHEt9)-LHRH also called Histrelin, is a potent LHRH agonist. Histrelin stimulates LH and FSH
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