Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dabigatran Etexilate Mesylate (BIBR 1048MS) 是一种口服具有活性的 Dabigatran 前药,具有抗凝作用,能够预防心房颤动引起的静脉血栓栓塞和中风。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 109 | 现货 | ||
2 mg | ¥ 143 | 现货 | ||
5 mg | ¥ 218 | 现货 | ||
10 mg | ¥ 328 | 现货 | ||
25 mg | ¥ 582 | 现货 | ||
50 mg | ¥ 892 | 现货 | ||
100 mg | ¥ 1,320 | 现货 | ||
200 mg | ¥ 1,930 | 现货 | ||
500 mg | ¥ 3,160 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 348 | 现货 |
产品描述 | Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM). |
靶点活性 | Thrombin-induced platelet aggregation:10 nM, Thrombin-induced platelet aggregation:4.5 nM (Ki) |
体外活性 | Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM), while showing no inhibitory effect on other platelet-stimulating agents. Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC50: 0.56 μM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 μM, respectively [1]. |
体内活性 | Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial hemorrhages and hemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2]. |
别名 | 甲磺酸达比加群酯, BIBR 1048MS, Dabigatran etexilate methanesulfonate |
分子量 | 723.84 |
分子式 | C34H41N7O5.CH4O3S |
CAS No. | 872728-81-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (69.08 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3815 mL | 6.9076 mL | 13.8152 mL | 34.538 mL |
5 mM | 0.2763 mL | 1.3815 mL | 2.763 mL | 6.9076 mL | |
10 mM | 0.1382 mL | 0.6908 mL | 1.3815 mL | 3.4538 mL | |
20 mM | 0.0691 mL | 0.3454 mL | 0.6908 mL | 1.7269 mL | |
50 mM | 0.0276 mL | 0.1382 mL | 0.2763 mL | 0.6908 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dabigatran Etexilate Mesylate 872728-81-9 Proteases/Proteasome Thrombin venousthromboembolism prodrug agent anticoagulant atrial Dabigatran fibrillation orally antithrombotic Inhibitor 甲磺酸达比加群酯 effects BIBR 1048MS active inhibit Dabigatran etexilate methanesulfonate Dabigatran etexilate inhibitor