Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 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 * 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: 25 mg/mL (53.71 mM), Sonication and heating are recommended.
DMSO: 20 mg/mL (42.97 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMF / DMSO | 1 mM | 2.1483 mL | 10.7416 mL | 21.4832 mL | 53.708 mL |
5 mM | 0.4297 mL | 2.1483 mL | 4.2966 mL | 10.7416 mL | |
10 mM | 0.2148 mL | 1.0742 mL | 2.1483 mL | 5.3708 mL | |
20 mM | 0.1074 mL | 0.5371 mL | 1.0742 mL | 2.6854 mL | |
DMF | 50 mM | 0.043 mL | 0.2148 mL | 0.4297 mL | 1.0742 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CVT-10216 1005334-57-5 Metabolism Dehydrogenase anxiolytic CVT 10216 inhibit 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 Aldehyde Dehydrogenase (ALDH) alcohol-preferring CVT10216 Inhibitor social interaction inhibitor