Identification | Back Directory | [Name]
2-Thiophenecarboxamide, 5-chloro-N-[(1R)-1-(methoxymethyl)-2-[[3-methyl-4-(3-oxo-4-morpholinyl)phenyl]amino]-2-oxoethyl]- | [CAS]
811811-33-3 | [Synonyms]
EMD 495235 2-Thiophenecarboxamide, 5-chloro-N-[(1R)-1-(methoxymethyl)-2-[[3 5-chloro-N-[(2R)-3-methoxy-1-[3-methyl-4-(3-oxomorpholin-4-yl)anilino]-1-oxopropan-2-yl]thiophene-2-carboxamide 2-Thiophenecarboxamide, 5-chloro-N-[(1R)-1-(methoxymethyl)-2-[[3-methyl-4-(3-oxo-4-morpholinyl)phenyl]amino]-2-oxoethyl]- | [Molecular Formula]
C20H22ClN3O5S | [MDL Number]
MFCD11656013 | [MOL File]
811811-33-3.mol | [Molecular Weight]
451.92 |
Hazard Information | Back Directory | [Uses]
EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC50 of 5.5 nM and a Ki of 6.8 nM. EMD 495235 shows anticoagulant activities[1]. | [in vivo]
EMD 495235 is characterized by rapid absorption from the gastrointestinal tract, plasma elimination half-lives of 0.57-2.3 h, a clearance between 0.25 and 1.3L/h/kg and absolute bioavailability of 60-80% in Wistar rats, Beagle dogs and Cynomolgus monkeys[1]. | [References]
[1] Werner W K R Mederski, et al. Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5817-22. DOI:10.1016/j.bmcl.2004.09.043 |
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