CVT-12012 是口服具有活性的硬脂酰-CoA 去饱和酶抑制剂,能够抑制大鼠微粒体和人 HEPG2 的活性,它们的IC50值分别为 38 nM,6.1 nM。
产品描述
CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).
体内活性
CVT-12012 is highly potent in a human cell-based (HEPG2) SCD assay (IC(50)=6nM). This compound has 78% oral bioavailability in rats and is preferentially distributed into liver (76 times vs plasma) with relatively low brain penetration[1].
Cas No.
1018675-35-8
分子式
C21H21F3N4O3
分子量
434.419
储存和溶解度
DMSO:125 mg/mL (287.75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years