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CVT-10216 是可逆的、选择性的醛脱氢酶 2(ALDH-2)抑制剂,IC50为 29 nM。对 ALDH-1的抑制作用较弱,IC50为 1.3 μM。 它可以减少偏爱酒精的大鼠过量饮酒,并表现出抗焦虑作用。
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CVT-10216 是可逆的、选择性的醛脱氢酶 2(ALDH-2)抑制剂,IC50为 29 nM。对 ALDH-1的抑制作用较弱,IC50为 1.3 μM。 它可以减少偏爱酒精的大鼠过量饮酒,并表现出抗焦虑作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 559 | 现货 | |
5 mg | ¥ 1,350 | 现货 | |
10 mg | ¥ 2,320 | 现货 | |
25 mg | ¥ 3,990 | 现货 | |
50 mg | ¥ 5,680 | 现货 | |
100 mg | ¥ 7,930 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,480 | 现货 |
产品描述 | 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. |
靶点活性 | ALDH2:29 nM |
体内活性 | CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 that reduces excessive alcohol drinking.?Anxiety plays a role in alcoholism. As reflected in social interaction behavior in four unrelated rodent models: endogenous anxiety-like behavior in na?ve Fawn-Hooded rats, repeated alcohol-withdrawal-induced anxiety, restraint stress-induced anxiety and drug-induced anxiety.?CVT-10216 counteracted anxiety in all models except that produced by the 5-HT(2C) agonist, mCPP.?CVT-10216 exhibited both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety.?Importantly, anxiogenic behavior induced by the benzodiazepine receptor inverse agonist, DMCM, was counteracted dose-dependently by CVT-10216.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. ?However it has no significant effects on locomotor activity. CVT-10216 (intraperitoneal injection; 3.75, 7.5, or 15 mg/kg) shows 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]. |
别名 | 3-[[[3-[4-[(甲基磺酰基)氨基]苯基]-4-氧代-4H-苯并吡喃-7-基]氧基]甲基]苯甲酸 |
分子量 | 465.48 |
分子式 | C24H19NO7S |
CAS No. | 1005334-57-5 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMF: 25 mg/mL (53.71 mM), Sonication and heating are recommended. DMSO: 20 mg/mL (42.97 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/DMF
DMF
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