CVT-12012,1018675-35-8

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CVT-12012

CAS No. : 1018675-35-8

MCE 国际站：CVT-12012

产品活性：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。

研究领域：Metabolic Enzyme/Protease

作用靶点：Stearoyl-CoA Desaturase (SCD)

In Vitro: CVT-12012 (Compound 5b) displays the highest potency in both the microsomal and the HEPG2 SCD assays (IC₅₀ 38 nM and 6.1 nM, respectively) compared to the other methyl-substituted compounds.

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.

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