JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively.
IC50&Target
IC50: 2 nM (FAAH), 4 nM (MAGL)
体外研究
JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC50 values of 13 and 19 nM, respectively).
JZL195 inhibits rat and human FAAH and MAGL enzymes with IC50 values in the range of ≈10-100 nM based on competitive ABPP assays.
体内研究
JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay.
Animal Model:
Male C57BL/6J mice
Dosage:
20 mg/kg
Administration:
Intraperitoneal injection
Result:
Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone.
分子式
C24H23N3O5
分子量
433.46
CAS号
1210004-12-8
运输条件
Room temperature in continental US; may vary elsewhere.