Betrixaban (PRT054021) hydrochloride 是一种有效的，具有口服活性的选择性Factor Xa(fXa) 抑制剂，IC50为 1.5 nM。Betrixaban hydrochloride 具有抗血栓形成效果。

Betrixaban (PRT054021) hydrochloride is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC 50 of 1.5 nM. Betrixaban hydrochloride shows antithrombotic effect [1] [3].

Betrixaban (PRT054021) shows IC 50 of 8.9 μM in patch clamp hERG assays [1]. Betrixaban shows an IC 50 and a K i of 6.3 μM and 3.5 μM for the plasma kallikrein, respectively [1]. Betrixaban (hERG K i 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG K i 0.5 μM) [1]. Betrixaban (5-25 ng/mL) inhibits thrombin generation [3].

Betrixaban (0.5 mg/kg, i.v.; 2.5 mg/kg, p.o.) has bioavailability of 51.6% in dog [1]. Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has bioavailability of 58.7% in monkey [1]. Betrixaban mediated whole-blood INR increase is reversed by r-Antidote. After i.v. infusion for 30 min, the total plasma concentrations of Betrixaban is 0.2±0.01 μM, and the percentages of unbound inhibitor is 40%±7.2%. After administration of r-Antidote, the total plasma concentration increased to 2.0±0.4 μM, and the percentage of unbound inhibitor declined to 0.3%±0.1% [2]. Betrixaban (3 mg/kg) shows nearly comparable inhibition of thrombus mass to enoxaparin 1.6 mg/kg (76% vs 96% inhibition) in the rabbit abdominal vena cava model of clot accretion on cotton threads [3]. Betrixaban (19.1 mg/kg) is at least as effective at maintaining patency as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d (90% vs 70% vs 80% patency, respectively) in the ferric chloride injury model of rodent carotid artery [3].

2099719-47-6

C23H23Cl2N5O3

488.37

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years