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CVT-10216 is a Potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50: 29 nM). CVT-10216 also has inhibitory effect of ALDH-1 (IC50: 1.3 μM). CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.