CVT-12012

Names

[ Name ]:
CVT-12012

[Synonym ]:
unii-oh3j29q653

Biological Activity

[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.

[Related Small Molecules]

A939572 | PluriSln 1 | SCD inhibitor 1 | CAY 10566 | MK-8245 | XEN723

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₁F₃N₄O₃

[ Molecular Weight ]:
434.41200

[ Exact Mass ]:
434.15700

[ PSA ]:
99.74000

[ LogP ]:
3.35760

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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