CVT-10216

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、高选择性、可逆的 ALDH2 抑制剂，IC50 为 29 nM，对 ALDH1 无显着抑制作用 (IC50=1,300 nM)。

A potent, highly selective, reversible inhibitor of ALDH2 with IC50 of 29 nM, shows no significant inhibition for ALDH1 (IC50=1,300 nM); demonstrates therapeutic potential to reduce excessive drinking and to suppress relapse in abstinent alcoholics; also shows both anxiolytic and antidipsotropic properties in rats; selectively suppresses binge eating of palatable food and attenuates dopamine release in the accumbens of sugar-bingeing rats.Alcoholism Discontinued.

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CVT-10216 (intraperitoneal?injection; 3.75, 7.5, or 15 mg/kg) exhibits aincrease 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.

CVT 10216 | GS455534 | GS-455534

Metabolic Enzyme/Protease

ALDH

ALDH

Neurological Disease

Alcoholism

1005334-57-5

465.5

C24H19NO7S

>98% (HPLC)

In Vitro:?DMF : 25 mg/mL (53.71 mM加)

O=C(O)C1=CC=CC(COC2=CC=C3C(C(C4=CC=C(NS(=O)(C)=O)C=C4)=COC3=C2)=O)=C1

3-[[[3-[4-[(Methylsulfonyl)amino]phenyl]-4-oxo-4H-1-benzopyran-7-yl]oxy]methyl]benzoic acid

(-20℃)

With Ice Pack

≥ 2 years