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Dabigatran etexilate mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dabigatran etexilate mesylate图片
CAS NO:872728-81-9
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BIBR 1048MS
甲磺酸达比加群酯
Dabigatran etexilate methanesulfonate
产品介绍
Dabigatran etexilate mesylate 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。

产品描述

Dabigatran etexilate mesylate is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).

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].

Cas No.

872728-81-9

分子式

C35H45N7O8S

分子量

723.85

别名

BIBR 1048MS;甲磺酸达比加群酯;Dabigatran etexilate methanesulfonate

储存和溶解度

DMSO:50 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years