Formulation: A crystalline solid
Formal Name: 6-[1-(phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-1-9-luteinizing hormone-releasing factor (swine), acetate
Purity: ≥98%
Formula Markup: C66H86N18O12 • XC2H4O2
Formula Weight: 1323,5
Shelf life (days): 1460
CAS Number: 220810-26-4
Notes: 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).{36464} It stimulates release of oxytocin (Item No. 11799) and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM.{36469,36470} 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.{36471} Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty.
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