Razaxaban hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性、口服生物可利用的 Xa 因子 (FXa) 抑制剂，Ki 为 o.19 nM。

A highly potent, selective, and orally bioavailable factor Xa (FXa) inhibitor with Ki of o.19 nM, >5,000-fold selectivity over a series of related serine proteases; inhibits thrombus formation in a dose-dependent manner with an ID50 of 1.6 μmol kg-1 h-1 in rabbit arterio-venous shunt thrombosis model.Thrombosis Phase 2 Discontinued.

Razaxaban (compound 11d) shows good Caco-2 permeability. The anticoagulant activity of Razaxaban (compound 11d) is evaluated in the in vitro human plasma activated partial thromboplastin time (aPTT) and human prothrombin time (PT) assays. Razaxaban shows a doubling of aPTT and PT at 6.1 μM and 2.1 μM, respectively. The human and rabbit plasma protein binding are found to be 90.5% and 93.4%, respectively, using equilibrium dialysis. Razaxaban is found to have similar affinity in the rabbit factor Xa assay with a Ki of 0.16 nM.

Razaxaban (Compound 11d; 0.21-9.4 mg/kg/hour; intravenous injection) inhibits thrombus formation in a dose-dependent manner with an ID50 of 1.6 μmol/kg/h in the rabbit arterio-venous shunt thrombosis model. Animal Model:Rabbit arterio-venous shunt thrombosis model Dosage:0.21 mg/kg/hour, 0.7 mg/kg/hour, 2.1 mg/kg/hour, 9.4 mg/kg/hour Administration:Intravenous injection Result:Inhibited thrombus formation in a dose-dependent manner with an ID50 of 1.6 μmol/kg/h.

DPC 906 | DPC906 | BMS-561389 | BMS561389

Metabolic Enzyme/Protease

Factor Xa

Factor Xa

Cardiovascular Disease

Thrombosis

405940-76-3

564.93

C24H21ClF4N8O2

>98% (HPLC)

——

CN(C)CC1=NC=CN1C2=CC(=C(C=C2)NC(=O)C3=CC(=NN3C4=CC5=C(C=C4)ON=C5N)C(F)(F)F)F.Cl

2-(3-amino-1,2-benzoxazol-5-yl)-N-[4-[2-[(dimethylamino)methyl]imidazol-1-yl]-2-fluorophenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide hydrochloride

(-20℃)

With Ice Pack

≥ 2 years