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- 产品描述： Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect
- 靶点： IC50: 1.5 nM (fXa) Ki: 0.117 nM (fXa), 1.8 μM (hERG)
- 体内研究： Betrixaban (0.5 mg/kg, i.v.; 2.5 mg/kg, p.o.) has oral bioavailability of 51.6% in dog. Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has oral bioavailability of 58.7% in monkey. 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%. 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. 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
- 参考文献：
1. Zhang P, et al. Discovery of Betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):21 2. Lu G, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51. 3. Chan NC, et al. Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism. Vasc Health Risk Manag. 2015 Jun 26;11:343-51.
- 溶解性： Soluble in DMSO
- 保存条件： 2-8℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.213 ml 11.064 ml 22.128 ml 5 mM 0.443 ml 2.213 ml 4.426 ml 10 mM 0.221 ml 1.106 ml 2.213 ml 50 mM 0.044 ml 0.221 ml 0.443 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
