CVT-10216是一种强效且选择性的醛脱氢酶-2(ALDH2)抑制剂,ALDH2 和 ALDH1 的 IC50 分别为 29 nM 和 1300 nM。
描述 | CVT-10216 is a highly selective, reversible inhibitor of aldehyde dehydrogenase-2 (ALDH-2) with an IC50 of 29 nM. Additionally, CVT-10216 exhibits inhibitory effects on ALDH-1 with an IC50 of 1.3 μM. CVT-10216 has demonstrated the ability to decrease excessive alcohol consumption in alcohol-preferring rats and to show anxiolytic effects [1]. |
体内研究 | When administered intraperitoneally at doses of 3.75, 7.5, or 15 mg/kg, CVT-10216 shows an increase in social interaction in a dose-dependent manner, with a notable 2-fold rise in social interaction observed after 15 mg/kg in Fawn-Hooded rats [1]. CVT-10216 (intraperitoneal injection; 3.75 or 15 mg/kg) was evaluated at 5 hours into the third withdrawal period. The anxiolytic effect of 15 mg/kg CVT-10216 was observed in this model, while no significant effects on locomotor activity were noted [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM | 2.15mL 0.43mL 0.21mL | 10.74mL 2.15mL 1.07mL | 21.48mL 4.30mL 2.15mL |
CAS号 | 1005334-57-5 |
分子式 | C24H19NO7S |
分子量 | 465.475 |
别名 | GS-455534 |
运输 | 蓝冰 |
存储条件 | 液体 -20°C:1个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 | DMSO: 18 mg/mL(38.67 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO DMF: 25 mg/mL(53.71 mM),配合低频超声助溶 |
动物实验配方 |