Betrixaban maleate - CAS:936539-80-9

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Betrixaban maleate (Synonyms:PRT054021 maleate;贝曲西班苹果酸盐)

目录号 : KM27114 CAS No. : 936539-80-9 纯度 : 98%

Data Sheet SDS 产品使用指南

Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect.

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect.

体外研究

Betrixaban (PRT054021) shows IC₅₀ of 8.9 μM in patch clamp hERG assays.
Betrixaban shows an IC₅₀ and a K_i of 6.3 μM and 3.5 μM for the plasma kallikrein, respectively.
Betrixaban (hERG K_i 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG K_i⩽0.5 μM).
Betrixaban (5-25 ng/mL) inhibits thrombin generation.

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.

分子式

C₂₇H₂₆ClN₅O₇

分子量

567.98

CAS号

936539-80-9

中文名称

贝曲西班苹果酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO: 50 mg/mL (88.03 mM; Need ultrasonic)

H2O : 2 mg/mL (3.52 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7606 mL	8.8031 mL	17.6063 mL
5 mM	0.3521 mL	1.7606 mL	3.5213 mL
10 mM	0.1761 mL	0.8803 mL	1.7606 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： 98%