Betrixaban

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. 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. 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.Formal Name: N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxy-benzamide. CAS Number: 330942-05-7. Synonyms: MK-4448, MLN1021, PRT054021. Molecular Formula: C23H22ClN5O3. Formula Weight: 451.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 289 nm. SMILES: ClC1=CC=C(NC(C2=CC(OC)=CC=C2NC(C3=CC=C(C(N(C)C)=N)C=C3)=O)=O)N=C1. InChi Code: InChI=1S/C23H22ClN5O3/c1-29(2)21(25)14-4-6-15(7-5-14)22(30)27-19-10-9-17(32-3)12-18(19)23(31)28-20-11-8-16(24)13-26-20/h4-13,25H,1-3H3,(H,27,30)(H,26,28,31). InChi Key: XHOLNRLADUSQLD-UHFFFAOYSA-N.