CAS:1210004-12-8JZL 195

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JZL195 functions as a dual inhibitor of FAAH and MAGL with IC50 of 13 nM and 19 nM respectively in brain of mouse.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1210004-12-8

储存条件

分子式

C24H23N3O5

运输

蓝冰

分子量

433.46

别名

溶解度

DMSO	37.0 mg/mL (85.4 mM) warming
Water	insoluble

动物实验配方

生物活性

描述JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 values of 2nM and 4nM, respectively. It exhibited broad activity in the tetrad test for CB1 agonism, causing analgesia, hypomotilty, and catalepsy. Male C57BL/6 mice administered JZL195 at doses ranging in 3–20mg/kg, i.p., for 4h showed dose-dependent reductions in brain FAAH, MAGL, and ABHD6 activities as judged by gel-based ABPP that correlated with near-complete inhibition of both AEA and 2-AG hydrolysis. JZL195 reduced inflammation induced allodynia, mechanical allodynia and thermal hyperalgesia, as well as produced catalepsy and sedation in a dose dependent manner. It displays greater efficacy than FAAH or MAGL specific inhibitors.
动物研究
剂量
Mice: 5 mg/kg - 40 mg/kg^[3] (i.p.), 120 mg/kg^[4] (i.p.); 18 mg/kg, 30 mg/kg^[5] (s.c.)

给药途径
i.p., s.c.

动物研究
剂量	Mice: 5 mg/kg - 40 mg/kg^[3] (i.p.), 120 mg/kg^[4] (i.p.); 18 mg/kg, 30 mg/kg^[5] (s.c.)
给药途径	i.p., s.c.