CVT-12012 |
| Catalog No.GC31447 |
A stearoyl-CoA desaturase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1018675-35-8
Sample solution is provided at 25 µL, 10mM.
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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.
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 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].
[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.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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