Product Name :
CVT-12012
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.
CAS:
1018675-35-8
Molecular Weight:
434.41
Formula:
C21H21F3N4O3
Chemical Name:
2-hydroxy-N-2-[3-methyl-2-oxo-7-([3-(trifluoromethyl)phenyl]methylamino)-1,2-dihydroquinoxalin-1-yl]ethylacetamide
Smiles :
CC1=NC2C=CC(=CC=2N(CCNC(=O)CO)C1=O)NCC1C=C(C=CC=1)C(F)(F)F
InChiKey:
HRAQDVZJYIAWOV-UHFFFAOYSA-N
InChi :
InChI=1S/C21H21F3N4O3/c1-13-20(31)28(8-7-25-19(30)12-29)18-10-16(5-6-17(18)27-13)26-11-14-3-2-4-15(9-14)21(22,23)24/h2-6,9-10,26,29H,7-8,11-12H2,1H3,(H,25,30)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 1018675-35-8|Molecular Weight: 434.41|Formula: C21H21F3N4O3|Chemical Name: 2-hydroxy-N-2-[3-methyl-2-oxo-7-([3-(trifluoromethyl)phenyl]methylamino)-1,2-dihydroquinoxalin-1-yl]ethylacetamide|Smiles: CC1=NC2C=CC(=CC=2N(CCNC(=O)CO)C1=O)NCC1C=C(C=CC=1)C(F)(F)F|InChiKey: HRAQDVZJYIAWOV-UHFFFAOYSA-N|InChi: InChI=1S/C21H21F3N4O3/c1-13-20(31)28(8-7-25-19(30)12-29)18-10-16(5-6-17(18)27-13)26-11-14-3-2-4-15(9-14)21(22,23)24/h2-6,9-10,26,29H,7-8,11-12H2,1H3,(H,25,30)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 125 mg/mL (287.Futibatinib supplier 75 mM; Need ultrasonic).NNZ 2591 site |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:32940723 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.|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.|Products are for research use only. Not for human use.|
