1819357-88-4
中文名稱
化合物 T26988
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T26988 英文別名
CFM184CFM-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-
應(yīng)用領(lǐng)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).