1308378-95-1|SKI2496|(R)-4-((2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid|-范德生物科技公司

SKI2496

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names：
(R)-4-((2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid
CAS号：
1308378-95-1
MDL Number：
MF(分子式)： C35H36F7N5O5 MW(分子量)： 739.6918
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	(R)-4-((2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid
英文别名	SKI2496; SKI-2496; SKI 2496.
CAS号	1308378-95-1
Inchi	InChI=1S/C35H36F7N5O5/c1-22-31(45-17-15-44(16-18-45)19-24-12-13-29(52-24)35(40,41)42)32(50)47(21-28(23-7-3-2-4-8-23)43-14-6-11-30(48)49)33(51)46(22)20-25-26(34(37,38)39)9-5-10-27(25)36/h2-5,7-10,12-13,28,43H,6,11,14-21H2,1H3,(H,48,49)/t28-/m0/s1
InchiKey	JLKXURLUTOXXPN-NDEPHWFRSA-N
分子式 Formula	C35H36F7N5O5
分子量 Molecular Weight	739.6918
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	SKI2496(CAS:1308378-95-1):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	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 available hormonal therapy.
Application1
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警示图
危险性	Warning
危险性警示
安全声明
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备注

[1]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 HormoneReceptor Antagonist. J Med Chem. 2016 Sep 27. [Epub ahead of print] PubMed PMID:27608177.