产品简介：

Betrixaban 是一种口服有效的选择性factor Xa(fXa) 抑制剂，IC50为 1.5 nM。

别名：贝曲沙班
分子式：C₂₃H₂₂ClN₅O₃ 分子量：451.91
物理性状及指标：
外观：……………………粉末
溶解性：…………………DMSO:22mg/mL(48.68 mM; Need ultrasonic and warming)；H₂O：Insoluble
含量：……………………>98%

储存条件：

-20℃，避光防潮密闭干燥

运输条件：

2~8℃运输

生物活性
描述	Betrixaban is a new, long-acting, oral and selectiveFactor Xainhibitor that decreases prothrombinase activity and thrombin generation.
IC50& Target	Factor Xa (Cell-free assay)：1.5 nM
体外研究	In patch clamp hERG assays, Betrixaban has IC50of 8.9 μM. The plasma kallikrein IC50 and Kivalues for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽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.

储液配置
按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃ 1-3月；-80℃ 3-6月。
	1 mg	5 mg	10 mg
1 mM	2.2128 mL	11.0641 mL	22.1283 mL
5 mM	0.4426 mL	2.2128 mL	4.4257 mL
10 mM	0.2213 mL	1.1064 mL	2.2128 mL
50 mM	0.0443 mL	0.2213 mL	0.4426 mL