Opicapone is a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase.
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描述 | Opicapone (BIA 9-1067) serves as a potent third-generation catechol-O-methyltransferase (COMT) inhibitor, primarily utilized in Parkinson's disease and motor fluctuation research. It reduces cellular ATP content with an IC50 of 98 μM[1]. |
体内研究 | In rats, Opicapone inhibits peripheral COMT with ED50 values below 1.4 mg/kg up to 6 hours post-administration, sustaining its effect over 8 hours, and maintaining significant effects on plasma L-DOPA levels and brain catecholamines for up to 24 hours post-administration[1]. |
体外研究 | Opicapone exerts a prolonged inhibitory effect on peripheral COMT, thereby enhancing the bioavailability of L-DOPA without inducing toxicity. Additionally, it decreases mitochondrial membrane potential with an IC50 of 181 μM in human primary hepatocytes[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.42mL 0.48mL 0.24mL |
12.10mL 2.42mL 1.21mL |
24.20mL 4.84mL 2.42mL |
CAS号 | 923287-50-7 |
分子式 | C15H10Cl2N4O6 |
分子量 | 413.169 |
别名 | BIA 9-1067 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(254.13 mM),配合低频超声助溶,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 |
动物实验配方 |