Betrixaban hydrochloride(330942-05-7(free base)) 是一种有效的、选择性的、口服有效的 Xa 因子 (fXa) 抑制剂 (IC50: 1.5 nM)。

Betrixaban is a potent, selective, and orally efficacious factor Xa (fXa) inhibitor (IC50: 1.5 nM).

In patch clamp hERG assays, Betrixaban has IC50 of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki?0.5 μM)[1].

Betrixaban (0.5 mg/kg, i.v. and 2.5 mg/kg, p.o.) has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey[1]. Both Betrixaban and Apixa-ban-mediated whole-blood INR increases are similarly reversed by r-Antidote. After i.v. infusion of the three fXa inhibitors (each admin?istered individually) for 30 min, the total plasma concentrations of rivaroxaban, Betrixaban and apixaban are 1.4±0.4 μM (mean±s.d.), 0.2±0.01 μM and 1.4±0.3 μM, respectively, and the percentages of unbound inhibitor are 2.2%±0.8% (mean±s.d.), 40%±7.2% and 1.5%±0.3%, respectively. After administration of r-Antidote, the total plasma concentrations of the inhibitors increased to 1.9±0.09 μM, 2.0±0.4 μM and 4.2±0.7 μM, respectively, and the percentage of unbound inhibitor declined to 0%, 0.3%±0.1% and 0.05%±0.02%, respectively. Thus, for each of the three inhibitors, correction of prothrombin time by r-Antidote to near-normal values is associated with a reduction in the free fraction of the inhibitor[2].

T4690

C23H23Cl2N5O3

488.36

盐酸贝曲西班;PRT054021 hydrochloride

DMSO:20 mg/mL (44.26 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years