CVT-10216

• CAT Number: I006317
• CAS Number: 1005334-57-5
• Molecular Formula: C24H19NO7S
• Molecular Weight: 465.48
• Purity: ≥95%
• Synonyms: 3-[[3-[4-(methanesulfonamido)phenyl]-4-oxochromen-7-yl]oxymethyl]benzoic acid
• 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)
• InChIKey: YYOOFJZTRCPVFD-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)NC1=CC=C(C=C1)C2=COC3=C(C2=O)C=CC(=C3)OCC4=CC(=CC=C4)C(=O)O

CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects[1].
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[1].
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[1].

Reference

[1]. Overstreet DH, et al. A selective ALDH-2 inhibitor reduces anxiety in rats.Pharmacol Biochem Behav. 2009 Dec;94(2):255-61.
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