WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 530606
Description: 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.
MedKoo Cat#: 530606
Chemical Formula: C24H19NO7S
Exact Mass: 465.08822
Molecular Weight: 465.48
Elemental Analysis: C, 61.93; H, 4.11; N, 3.01; O, 24.06; S, 6.89
Synonym: CVT-10216; CVT 10216; CVT10216.
IUPAC/Chemical Name: 3-(((3-(4-(methylsulfonamido)phenyl)-4-oxo-4H-chromen-7-yl)oxy)methyl)benzoic acid
InChi Key: YYOOFJZTRCPVFD-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(O)C1=CC=CC(COC2=CC=C3C(C(C4=CC=C(NS(=O)(C)=O)C=C4)=COC3=C2)=O)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 465.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: 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.
2: 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.
3: 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.
4: Arolfo MP, Overstreet DH, Yao L, Fan P, Lawrence AJ, Tao G, Keung WM, Vallee BL, Olive MF, Gass JT, Rubin E, Anni H, Hodge CW, Besheer J, Zablocki J, Leung K, Blackburn BK, Lange LG, Diamond I. Suppression of heavy drinking and alcohol seeking by a selective ALDH-2 inhibitor. Alcohol Clin Exp Res. 2009 Nov;33(11):1935-44. doi: 10.1111/j.1530-0277.2009.01031.x. Epub 2009 Aug 10. PubMed PMID: 19673742.