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 |
CVT-12012 是一种有效的、具有口服活性的硬脂酰-CoA 去饱和酶 (SCD) 的抑制剂，其对大鼠微粒体和人 HEPG2 的 IC50 值分别为 38 nM，6.1 nM。
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 |