CS-2863
中文名称 | CS-2863 |
---|---|
中文同义词 | 化合物CVT-12012 |
英文名称 | CVT-12012 |
英文同义词 | CVT-12012;2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)phenyl]methylamino]quinoxalin-1-yl]ethyl]acetamide;CVT-2012;CS-2863;2-Hydroxy-N-(2-(3-methyl-2-oxo-7-(((3-(trifluoromethyl)phenyl)methyl)amino)-1,2-dihydroquinoxalin-1-yl)ethyl)acetamide;Acetamide, 2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[[3-(trifluoromethyl)phenyl]methyl]amino]-1(2H)-quinoxalinyl]ethyl]-;2-Hydroxy-N-[2-[3-methyl-2-oxo-7-[[[3-(trifluoromethyl)phenyl]methyl]amino]-1(2H)-quinoxalinyl]ethyl]acetamide;CVT 12012,Stearoyl-CoA Desaturase (SCD),inhibit,CVT12012,Inhibitor,CVT-12012 |
CAS号 | 1018675-35-8 |
分子式 | C21H21F3N4O3 |
分子量 | 434.41 |
EINECS号 | |
相关类别 | API |
Mol文件 | 1018675-35-8.mol |
结构式 | ![]() |
CS-2863 性质
密度 | 1.37±0.1 g/cm3(Predicted) |
---|---|
储存条件 | Store at -20°C |
溶解度 | DMF:30mg/mL; DMSO:30mg/mL; DMSO:PBS (pH 7.2) (1:6):0.14 mg/ml;乙醇:1mg/mL |
形态 | 结晶固体 |
酸度系数(pKa) | 13.29±0.10(Predicted) |
颜色 | 浅黄至黄色 |
IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2).
CVT-12012 (Compound 5b) displays the highest potency in both the microsomal and the HEPG2 SCD assays (IC 50 38 nM and 6.1 nM, respectively) compared to the other methyl-substituted compounds.
In a rat PK study, CVT-12012 demonstrates good oral bioavailability (78%). It appears that the oral absorption of CVT-12012 is not affected by a significant Pgp efflux, which is expected based on Caco-2 assay result. The plasma clearance of CVT-12012 is high (88 mL/min/kg) with elimination half-life of approximately 1 h.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-11034 | CVT-12012 | 1 mg | 400元 | |
2024/08/19 | HY-11034 | CS-2863 CVT-12012 | 1018675-35-8 | 5mg | 1000元 |