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)
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CVT-12012
CAS number：1018675-35-8(DMSO) molecular formula：C21H21F3N4O3
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1018675-35-8(DMSO) | molecular formula | C21H21F3N4O3 |
| molecular weight | 434.41 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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