中文名 | 贝曲西班 |
英文名 | Betrixaban |
别名 | 贝曲西班 贝曲沙班 贝曲沙班-D4 FXA抑制剂(BETRIXABAN) N-(5-氯-2-吡啶基)-2-(4-(N,N-二甲基甲脒基苯甲酰氨基)-5-甲氧基苯甲酰胺 N-(5-氯吡啶-2-基)-2-(4-(N,N-二甲基氨基甲酰基)苯甲酰胺基)-5-甲氧基苯甲酰胺 |
英文别名 | Betrixaban PRT 054021 Betrixaban, PRT-054021 N-(5-chloropyridin-2-yl)-2-(4-(N,N-diMethylcarbaMiMidoyl)benzaMido)-4-MethoxybenzaMide N-(5-Chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide N-(5-Chloro-2-pyridinyl)-2-[[4-[(diMethylaMino)iMinoMethyl]benzoyl]aMino]-5-MethoxybenzaMide 1-C-{4-[aMino(diMethylaMino)Methyl]benzene}-2-N-(5-chloropyridin-2-yl)-4-Methoxybenzene-1,2-dicarboxaMide |
CAS | 330942-05-7 |
EINECS | 682-459-2 |
化学式 | C23H22ClN5O3 |
分子量 | 451.91 |
密度 | 1.30±0.1 g/cm3(Predicted) |
熔点 | 210-213°C |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
酸度系数 | 11.00±0.70(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | Off-White |
体外研究 | In patch clamp hERG assays, Betrixaban has IC 50 of 8.9 μM. The plasma kallikrein IC 50 and K i values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG K i 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG K i ⩽0.5 μM). |
体内研究 | Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey. Both Betrixaban and Apixa-ban-mediated whole-blood INR increases are similarly reversed by r-Antidote. After i.v. infusion of the three fXa inhibitors (each admin¬istered individually) for 30 min, the total plasma concentrations of rivaroxaban, Betrixaban and apixaban are 1.4±0.4 μM (mean±s.d.), 0.2±0.01 μM and 1.4±0.3 μM, respectively, and the percentages of unbound inhibitor are 2.2%±0.8% (mean±s.d.), 40%±7.2% and 1.5%±0.3%, respectively. After administration of r-Antidote, the total plasma concentrations of the inhibitors increased to 1.9±0.09 μM, 2.0±0.4 μM and 4.2±0.7 μM, respectively, and the percentage of unbound inhibitor declined to 0%, 0.3%±0.1% and 0.05%±0.02%, respectively. Thus, for each of the three inhibitors, correction of prothrombin time by r-Antidote to near-normal values is associated with a reduction in the free fraction of the inhibitor. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.213 ml | 11.064 ml | 22.128 ml |
5 mM | 0.443 ml | 2.213 ml | 4.426 ml |
10 mM | 0.221 ml | 1.106 ml | 2.213 ml |
5 mM | 0.044 ml | 0.221 ml | 0.443 ml |
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