Betrixaban (PRT054021) 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 具有抗血栓形成效果。
| 生物活性 | 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& Target | IC50: 1.5 nM (fXa)[1]
Ki: 0.117 nM (fXa), 1.8 μM (hERG)[1] |
体外研究
(In Vitro) | Betrixaban (PRT054021) shows IC50of 8.9 μM in patch clamp hERG assays[1].
Betrixaban shows an IC50and a Kiof 6.3 μM and 3.5 μM for the plasma kallikrein, respectively[1].
Betrixaban (hERG Ki1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki?0.5 μM)[1].
Betrixaban (5-25 ng/mL) inhibits thrombin generation[3].
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体内研究
(In Vivo) | 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].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(55.32 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2128 mL | 11.0641 mL | 22.1283 mL | | 5 mM | 0.4426 mL | 2.2128 mL | 4.4257 mL | | 10 mM | 0.2213 mL | 1.1064 mL | 2.2128 mL |
*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。 In Vivo: 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。 *以上所有助溶剂都可在本网站选购。
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