1018675-35-8

1018675-35-8 structure

Name: CVT-12012
Chemical Name: 2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)phenyl]methylamino]quinoxalin-1-yl]ethyl]acetamide
CAS Number: 1018675-35-8
Molecular Formula: C₂₁H₂₁F₃N₄O₃
Molecular Weight: 434.41200
Catalog: Signaling Pathways Metabolic Enzyme/Protease Stearoyl-CoA Desaturase (SCD)
Create Date: 2017-11-05 08:30:33
Modify Date: 2024-01-12 12:02:48
CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

Name	2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)phenyl]methylamino]quinoxalin-1-yl]ethyl]acetamide
Synonyms	unii-oh3j29q653

Description	CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Stearoyl-CoA Desaturase (SCD) Research Areas >> Metabolic Disease
Target	IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2)[1][2].
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[1].
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[1].
References	[1]. Koltun DO, et al. Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. [2]. Atkinson KA, et al. N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5.

1018675-34-7

1018675-35-8

Precursor 1
1018675-34-7
DownStream 0