| Description | CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells). |
| In vivo | CVT-12012 is highly potent in a human cell-based (HEPG2) SCD assay (IC(50)=6nM). This compound has 78% oral bioavailability in rats and is preferentially distributed into liver (76 times vs plasma) with relatively low brain penetration[1]. |
| Target activity | HepG2 cells:6.1 nM, Microsomal (rat):38 nM |
| molecular weight | 434.41 |
| Molecular formula | C21H21F3N4O3 |
| CAS | 1018675-35-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (287.75 mM) |
| References | 1. Koltun D O , Vasilevich N I , Parkhill E Q , et al. Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors[J]. Bioorganic and Medicinal Chemistry Letters, 2009, 19(11):3050-3053. 2. Atkinson KA, Beretta EE, Brown JA,et al.N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors[J].Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5. |