CVT-10216

CVT-10216 is a Potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50 values are 29 and 1300 nM for ALDH2 and ALDH1, respectively). CVT-10216 increases acetaldehyde after alcohol gavage and inhibits 2-bottle choice alcohol intake in heavy drinking rodents, including deprivation-induced drinking. Moreover, CVT-10216 also prevents operant self-administration and eliminates cue-induced reinstatement of alcohol seeking even when alcohol is not available (i.e., no acetaldehyde). Alcohol stimulates DA release in the NAc, which is thought to contribute to increased drinking and relapse in alcoholism. CVT-10216 prevents alcohol-induced increases in NAc DA without changing basal levels.

Product information

CAS Number: 1005334-57-5

Molecular Weight: 465.48

Formula: C24H19NO7S

Synonym:

CVT 10216

CVT10216

CVT-10216

Chemical Name: 3-(((3-(4-(methylsulfonamido)phenyl)-4-oxo-4H-chromen-7-yl)oxy)methyl)benzoic acid

Smiles: CS(=O)(=O)NC1C=CC(=CC=1)C1=COC2=CC(=CC=C2C1=O)OCC1C=CC=C(C=1)C(O)=O

InChiKey: YYOOFJZTRCPVFD-UHFFFAOYSA-N

InChi: InChI=1S/C24H19NO7S/c1-33(29,30)25-18-7-5-16(6-8-18)21-14-32-22-12-19(9-10-20(22)23(21)26)31-13-15-3-2-4-17(11-15)24(27)28/h2-12,14,25H,13H2,1H3,(H,27,28)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

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.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vivo:

CVT-10216 (intraperitoneal injection; 3.75, 7.5, or 15 mg/kg) exhibits a increase in social interaction as a dose-dependent manner, punctuated by a 2-fold increase in social interaction after 15 mg/kg in Fawn-Hooded rats. CVT-10216 (intraperitoneal injection; 3.75 or 15 mg/kg) are determined 5 h into the third withdrawal.It has the anxiolytic effect of 15 mg/kg CVT-10216 in this model, but has no significant effects on locomotor activity.

References:

1. Rezvani AH, Lawrence AJ, Arolfo MP, Levin ED, Overstreet DH. Novel medication targets for the treatment of alcoholism: preclinical studies. Recent Pat CNS Drug Discov. 2012 Aug;7(2):151-62. Review. PubMed PMID: 22574676.
2. Overstreet DH, Knapp DJ, Breese GR, Diamond I. A selective ALDH-2 inhibitor reduces anxiety in rats. Pharmacol Biochem Behav. 2009 Dec;94(2):255-61. doi: 10.1016/j.pbb.2009.09.004. Epub 2009 Sep 10. PubMed PMID: 19747934; PubMed Central PMCID: PMC2859712.
3. Bocarsly ME, Hoebel BG, Paredes D, von Loga I, Murray SM, Wang M, Arolfo MP, Yao L, Diamond I, Avena NM. GS 455534 selectively suppresses binge eating of palatable food and attenuates dopamine release in the accumbens of sugar-bingeing rats. Behav Pharmacol. 2014 Apr;25(2):147-57. doi: 10.1097/FBP.0000000000000029. PubMed PMID: 24603339.

Products are for research use only. Not for human use.