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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
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 | ¥ 538 | 现货 | |
| 5 mg | ¥ 1,330 | 现货 | |
| 10 mg | ¥ 2,290 | 现货 | |
| 25 mg | ¥ 3,990 | 现货 | |
| 50 mg | ¥ 5,680 | 现货 | |
| 100 mg | ¥ 7,920 | 现货 | |
| 200 mg | ¥ 10,600 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,370 | 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 |
| Smiles | CS(=O)(=O)Nc1ccc(cc1)-c1coc2cc(OCc3cccc(c3)C(O)=O)ccc2c1=O |
| 密度 | 1.468 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 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. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+90% Corn Oil: 2 mg/mL (4.3 mM), Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/DMF
DMF
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多