A Factor Xa inhibitor (Ki = 0.117 nM; IC50 = 1.5 nM); selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM); inhibits thrombin generation in a tissue factor-induced thrombin generation assay (5-25 ng/mL); inhibits thrombus mass formation 76% in a rabbit clot accretion model (3 mg/kg)

Betrixaban – 250 mg

Brand:
Cayman
CAS:
330942-05-7
Storage:
-20
UN-No:
Non-Hazardous - /

Betrixaban is an inhibitor of the serine protease Factor Xa (Ki = 0.117 nM; IC50 = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade.{36456} It is selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro, betrixaban inhibits thrombin generation when used at concentrations ranging from 5 to 25 ng/mL in a tissue factor-induced thrombin generation assay.{36457} In vivo, it inhibits thrombus mass formation by 76% in a rabbit clot accretion model when used at a dose of 3 mg/kg. Formulations containing betrixaban have been used as anticoagulants in the treatment and prevention of venous thromboembolism.{36458}  

 

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Description

A Factor Xa inhibitor (Ki = 0.117 nM; IC50 = 1.5 nM); selective for Factor Xa over hERG channels (Ki = 1.8 µM; IC50 = 8.9 µM); inhibits thrombin generation in a tissue factor-induced thrombin generation assay (5-25 ng/mL); inhibits thrombus mass formation 76% in a rabbit clot accretion model (3 mg/kg)

Formal name: N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxy-benzamide

Synonyms:  MK-4448|MLN1021|PRT054021

Molecular weight: 451.9

CAS: 330942-05-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Blood Coagulation Factors||Research Area|Cardiovascular System|Blood|Acute Phase Reactants||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Blood|Thrombosis

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