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 VitroCVT-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 VivoIn 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.Form:SolidIC50& Target:IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2). Specification: 0.99 Molecular Formula: C21H21F3N4O3 Molecular Weight: 434.41 PubChem CID: 25195516 Isomeric SMILES: CC1=NC2=C(C=C(C=C2)NCC3=CC(=CC=C3)C(F)(F)F)N(C1=O)CCNC(=O)CO
- UPC:
- 51172166
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- C649842-50mg
- CAS:
- 1018675-35-8
- Product Size:
- 50mg
