Dabigatran etexilate mesylate
甲磺酸达比加群酯
Catalog No.
A3345
凝血酶抑制剂,抗凝剂,dabigatran的前药
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Description:
IC50 Value: 4.5nM (Ki); 10nM(Thrombin-induced platelet aggregation) [1]
Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug,dabigatran etexilate.
in 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
Storage | Store at -20°C |
M.Wt | 723.84 |
Cas No. | 872728-81-9 |
Formula | C35H45N7O8S |
Synonyms | Pradaxa;BIBR 1048MS;Dabigatran etexilate methanesulfonate |
Solubility | ≥36.19 mg/mL in DMSO; insoluble in H2O; ≥45.8 mg/mL in EtOH with gentle warming |
Chemical Name | ethyl 3-(2-(((4-(N-((hexyloxy)carbonyl)carbamimidoyl)phenyl)amino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate methanesulfonate |
SDF | Download SDF |
Canonical SMILES | CCCCCCOC(NC(C1=CC=C(NCC2=NC3=C(C=CC(C(N(C4=CC=CC=N4)CCC(OCC)=O)=O)=C3)N2C)C=C1)=N)=O.CS(=O)(O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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