1819357-88-4

中文名称化合物 T26988

英文名称 Benzamide, N-[(1R,4R,7S)-2-(3-amino-4-chloroisoxazolo[5,4-c]pyridin-7-yl)-2-azabicyclo[2.2.1]hept-7-yl]-2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)-, rel-

CAS 1819357-88-4

分子式 C22H20Cl2N8O2

分子量 499.35

MOL 文件 1819357-88-4.mol

1819357-88-4 结构式

基本信息应用领域

基本信息

中文别名

化合物 T26988

英文别名

CFM184
CFM-184
CFM 184
Benzamide, N-[(1R,4R,7S)-2-(3-amino-4-chloroisoxazolo[5,4-c]pyridin-7-yl)-2-azabicyclo[2.2.1]hept-7-yl]-2-chloro-4-(3-methyl-1H-1,2,4-triazol-1-yl)-, rel-

应用领域

用途一

CFM-184 is an orally active factor IXa inhibitor with hFIXa IC50 = 4.9 nM; hPPB fu 4.1%, aPPT Ct2 = 5.8 uM (human). CFM-184 demonstrated excellent FIXa inhibitory potency, significant selectivity of hFIXa over hFXa (>6300-fold), reasonable anticoagulant efficacy on in vitro aPTT, and no effect on PT up to 200 μM. Regarding physicochemical and ADMET profiles14, CFM-184 showed moderate aqueous solubility, good membrane permeability, microsomal stability, and unbound fractions in plasma. PK studies of CFM-184 indicated moderate bioavailability in rats (51%) and reasonable half-life (0.8 hr in rats, 4.7 hr in dogs).