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
密度
1.37±0.1 g/cm3(Predicted)
酸度系数(pKa)
13.29±0.10(Predicted)
生物活性
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。
靶点
IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2).
体外研究
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.
体内研究
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.
