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.
性状
Solid
IC50 & Target[1][2]
IC50: 2 nM (FAAH), 4 nM (MAGL)
体外研究(In Vitro)
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
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.