SKU : MC502212
CAS Number : 1018675-35-8
Molecular Formula : C21H21F3N4O3 | Molecular Weight : 434.41
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | CVT-12012 |
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CAS Number | 1018675-35-8 |
MDL Number | MFCD18251587 |
Molecular Formula | C21H21F3N4O3 |
Molecular Weight | 434.41 |
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. IC50 & 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].
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