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| 产品描述 |
| 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. |
| 化学结构 |
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| 化学名称 |
| (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 |
| SMILES Code |
| O=C1C(N2CCN(CC3=CC=C(C(F)(F)F)O3)CC2)=C(C)N(CC4=C(C(F)(F)F)C=CC=C4F)C(N1C[C@H](NCCCC(O)=O)C5=CC=CC=C5)=O |
| 基本信息 |
产品编号:XM352
产品名称:SKI2496
CAS#:1308378-95-1
分子式:C35H36F7N5O5
精确分子量:739.2605
分子量:739.6918
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| 物化性质 |
外观: 白色或类白色固体粉末
纯度: >98%
运输信息: 非危险化学品，适于常温或冰袋运输。
储存条件: 低温，干燥，避光。
溶解性: 溶于DMSO, 不溶于水
储存期限: 3 年 -20℃ 固体储存 2 年 -80℃ 溶液储存 |
该产品只供科研使用，不能给病人提供。
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