Histrelin (acetate) (Synonyms: Des-Gly10,D-His(Bzl)6-LHRHethyl amide, Des-Gly10,D-His(Bzl)6,Pro-NHEt9-LHRH, (ImBzl)-d-His6,Pro9-NET-LHRH) |
| カタログ番号GC43866 |
ヒストレリンは、合成ゴナドトロピン放出ホルモン（GNRH）アゴニストであり、GNRH受容体（GNRHR；人間の受容体を発現するCHO細胞におけるKi = 0.2 nM）に結合します。
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Cas No.: 220810-26-4
Sample solution is provided at 25 µL, 10mM.
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Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor). It stimulates release of oxytocin and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM. In vivo, the initial dose of histrelin (100 μg) stimulates acute increases in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone serum levels (50-, 2.5-, and 15-fold, respectively), while chronic treatment leads to 95% decreases in LH and FSH responses in rhesus monkeys. Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty.
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