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产品描述 |
INCB3284 is a potent, selective, and orally bioavailable hCCR2 Antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates. In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h). |
化学结构 |
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化学名称 |
N-(2-(((R)-1-((1r,4R)-4-hydroxy-4-(6-methoxypyridin-3-yl)cyclohexyl)pyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide dimethanesulfonate |
SMILES Code |
O[C@]1(C2=CN=C(OC)C=C2)CC[C@@H](N3C[C@H](NC(CNC(C4=CC(C(F)(F)F)=CC=C4)=O)=O)CC3)CC1.CS(=O)(O)=O.CS(=O)(O)=O |
基本信息 |
产品编号:XM391 产品名称:INCB3284 mesylate 别名:INCB3284; INCB 3284; INCB-3284; INCB3284 mesylate; INCB3284 dimesylate. CAS#:887401-93-6 (mesylate); 887401-92-5 (free base). 分子式:C28H39F3N4O10S2 分子量:712.7532
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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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