Betrixaban (PRT054021) is a highly potent, selective, and orally efficaciousfactor Xa(fXa) inhibitor with anIC₅₀of 1.5 nM. Betrixaban shows antithrombotic effect^[1][3].

IC50: 1.5 nM (fXa)^[1]
Ki: 0.117 nM (fXa), 1.8 μM (hERG)^[1]

Betrixaban (PRT054021) shows IC₅₀of 8.9 μM in patch clamp hERG assays^[1].
Betrixaban shows an IC₅₀and a K_iof 6.3 μM and 3.5 μM for the plasma kallikrein, respectively^[1].
Betrixaban (hERG K_i1.8 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 oral bioavailability of 51.6% in dog^[1].
Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has oral 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].

451.91

Solid

C₂₃H₂₂ClN₅O₃

330942-05-7

贝曲西班

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(55.32 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.53 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液