Dabigatran产品描述：Dabigatran(BIB-953; BIBR 953ZW)是可逆的高活性直接凝血酶抑制剂（DTI），Ki为4.5 nM。
Dabigatran产品描述：Dabigatran(BIB-953; BIBR 953ZW) is a reversible ａnd selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]Target: thrombinin vitro: Dabigatran selectively ａnd reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 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 (IC(50): 0.56 microM). 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 microM, respectively [1]. in vivo: 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 haemorrhages ａnd haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics ａnd Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

研究领域：Membrane Transporter/Ion Channel

靶点：Calcium Channel

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Alternative_Names:BIBR 953;BIBR 953ZW

MWt:471.51

Formula:C25H25N7O3

SMILES:N=C(N)C(C=C1)=CC=C1NCC2=NC3=CC(C(N(CCC(O)=O)C4=NC=CC=C4)=O)=CC=C3N2C

Research_Area:Cardiovascular Disease



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