[CAS NO. 1018675-35-8] CVT-12012
PRODUCTS SPECIFICATIONS [1018675-35-8]
DESCRIPTION [1018675-35-8]
Overview
| MDL | MFCD18251587 |
|---|---|
| Molecular Weight | 434.41 |
| Molecular Formula | C21H21F3N4O3 |
| SMILES | O=C(NCCN1C(C(C)=NC2=C1C=C(NCC3=CC=CC(C(F)(F)F)=C3)C=C2)=O)CO |
Summary
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 [1] .
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 287.75 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3020 mL | 11.5099 mL | 23.0197 mL |
| 5 mM | 0.4604 mL | 2.3020 mL | 4.6039 mL |
| 10 mM | 0.2302 mL | 1.1510 mL | 2.3020 mL |
References
- [1] Koltun DO, et al. Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4.
- [2] Atkinson KA, et al. N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5.