CVT-12012
Names
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]:
[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]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C21H21F3N4O3
[ Molecular Weight ]:
434.41200
[ Exact Mass ]:
434.15700
[ PSA ]:
99.74000
[ LogP ]:
3.35760
[ Storage condition ]:
2-8℃