CVT-12012

小分子

CVT-12012

C656018-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC 50 s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively. In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2)

CVT-12012 是一种强效且可口服的硬脂酰-coA 去饱和酶 (SCD) 抑制剂，对大鼠微粒体和人类 HEPG2 的 IC 50 s 分别为 38 nM 和 6.1 nM。

1018675-35-8(DMSO)

C21H21F3N4O3

434.41 g/mol

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