SKI2496 is a potent and orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist (hGnRHR IC50 = 0.46 nM; max. LH inh. inh. (%, h)= 84%, 12h; LH inh. (24h) = 76%.). SKI2496 exhibited more selective antagonistic activity toward the human GnRH receptors over the GnRHRs in monkeys and rats, and SKI2496 also showed inhibitory effects on GnRH-mediated signaling pathways. Pharmacokinetic and pharmacodynamic evaluations of SKI2496 revealed improved bioavailability and superior gonadotropic suppression activity compared with Elagolix, the most clinically advanced compound. SKI2496 may represent a promising candidate for an orally bioavailable hormonal therapy. References: Kim SM, Lee M, Lee SY, Park E, Lee SM, Kim EJ, Han MY, Yoo T, Ann J, Yoon S, Lee J, Lee J. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Sep 27. [Epub ahead of print] PubMed PMID: 27608177.

纯度：≥98%

CAS：1308378-95-1