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。


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| 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]. |
| Administration | Dosage | Frequency | Description | References | ||
| Rats | Fawn-Hooded (FH) rats, alcohol-preferring (iP) rats, Sprague-Dawley (SD) rats | Intraperitoneal injection | 3.75, 7.5, 15 mg/kg | Single dose or multiple doses (e.g., prophylactic dosing in alcohol withdrawal models) | CVT-10216 exhibited anxiolytic effects in multiple anxiety models, including innate anxiety in FH rats, alcohol withdrawal-induced anxiety, restraint stress-induced anxiety, and DMCM-induced anxiety. CVT-10216 was ineffective against mCPP-induced anxiety. | Pharmacol Biochem Behav. 2009 Dec;94(2):255-61 |
| 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 |
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| CAS号 | 1005334-57-5 |
| 分子式 | C24H19NO7S |
| 分子量 | 465.48 |
| SMILES Code | O=C2C1=CC=C(OCC4=CC(C(O)=O)=CC=C4)C=C1OC=C2C3=CC=C(NS(=O)(C)=O)C=C3 |
| MDL No. | MFCD18072197 |
| 别名 | GS-455534 |
| 运输 | 蓝冰 |
| InChI Key | YYOOFJZTRCPVFD-UHFFFAOYSA-N |
| Pubchem ID | 23661666 |
| 存储条件 |
In solvent -20°C: 1个月 -80°C: 12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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