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贝曲西班 促销  ≥98% (HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(20mg/ml)
产品描述：基本信息 产品编号： B10023 产品名称： Betrixaban CAS: 330942-05-7   储存条件 粉末 -20℃ 四年     分子式： C23H22ClN5O3 溶于液体 -80℃ 两年 分子量 451.91 -20℃ 一个月 化学名：  N-(5-CHLOROPYRIDIN-2-YL)-2-(4-(N,N-DIMETHYLCARBAMIMIDOYL)BENZAMIDO)-5-METHOXYBENZAMIDE Solubility (25°C)：   体外:   DMSO 35mg/mL(77.44mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(5.53mM);Clear solution 此⽅案可获得≥2.5mg/mL(5.53mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.2128mL 11.0641mL 22.1283mL 5mM 0.4426mL 2.2128mL 4.4257mL 10mM 0.2213mL 1.1064mL 2.2128mL 50mM 0.0443mL 0.2213mL 0.4426mL   生物活性 产品描述 一种口服有效的选择性的factor Xa (fXa)抑制剂。 靶点 Factor Xa (Cell-free assay) 1.5nM 体外研究 In patch clamp hERG assays, Betrixaban has IC50 of 8.9μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3μM and 3.5μM respectively. Betrixaban (hERG Ki 1.8μM) exhibits significantly lower hERG activity than all the others (hERG Ki 0.5μM) 体内研究 Dosed at 0.5mg/kg IV and 2.5mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75mg/kg IV and 7.5mg/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±0.4μM (mean±s.d.), 0.2±0.01μM and 1.4±0.3μM, 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±0.09μM, 2.0±0.4μM and 4.2±0.7μM, 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 nearnormal values is associated with a reduction in the free fraction of the inhibitor   推荐实验方法(仅供参考) Animal Administration Rats Whole-blood INR values (mean±s.d.) in rats infused with Betrixaban (1mg/kg per hour) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6mg) over 5 min plus infusion (9mg/h) for up to 90 min. Circles, vehicle+vehicle; squares, Betrixaban + vehicle; triangles, Betrixaban + r-Antidote. *P≤0.02 compared to the r-Antidote treatment group determined by unpaired two-tailed t test. Whole-blood INR values (mean±s.d.) in rats infused with Apixaban (0.5mg per kg body weight h−1) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6mg) over 5 min plus infusion (6mg/h) for up to 90 min. Circles, vehicle + vehicle; squares, apixaban + vehicle; triangles, apixaban+r-Antidote. *P≤0.01 compared to the r-Antidote treatment group determined by unpaired two-tailed t test.
保存条件：-20℃

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