| Identification | Back Directory | [Name]
CVT-12012 | [CAS]
1018675-35-8 | [Synonyms]
CS-2863
CVT-2012
CVT-12012
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)phenyl]methylamino]quinoxalin-1-yl]ethyl]acetamide
2-Hydroxy-N-[2-[3-methyl-2-oxo-7-[[[3-(trifluoromethyl)phenyl]methyl]amino]-1(2H)-quinoxalinyl]ethyl]acetamide
Acetamide, 2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[[3-(trifluoromethyl)phenyl]methyl]amino]-1(2H)-quinoxalinyl]ethyl]-
2-Hydroxy-N-(2-(3-methyl-2-oxo-7-(((3-(trifluoromethyl)phenyl)methyl)amino)-1,2-dihydroquinoxalin-1-yl)ethyl)acetamide | [Molecular Formula]
C21H21F3N4O3 | [MOL File]
1018675-35-8.mol | [Molecular Weight]
434.41 |
| Chemical Properties | Back Directory | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
13.29±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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. | [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]. | [storage]
Store at -20°C | [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. DOI:10.1016/j.bmcl.2009.06.017
[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. DOI:10.1016/j.bmcl.2011.01.113 |
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| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|