JZL184 is an irreversible inhibitor for monoacylglycerol lipase (MAGL), the primary enzyme responsible for degrading the endocannabinoid 2-arachidonoylglycerol (2-AG). [1]

JZL 184 is a potent and selective inhibitor of monoacylglycerol lipase (MAGL) that displays IC 50 values of 8 nM and 4 µM for inhibition of MAGL and fatty acid amide hydrolase in mouse brain membranes, respectively. 1 When administered to mice at 16 mg/kg, intraperitoneally, JZL 184 reduces MAGL activity by 85%, elevates brain 2- AG levels by 8-...

2021年5月1日 · Using LC-MS, significantly increased 2-AG levels were detected in A549 cells treated with the MAGL inhibitor JZL184. In athymic nude mice, JZL184 suppressed metastasis of A549 cells in a dose-dependent manner, whereby the antimetastatic effect was cancelled by the CB 1 receptor antagonist AM-251.

2015年4月28日 · JZL184 treatment induced a significant decrease in expression levels of inflammation-induced, Iba1-immunoreactive microglia in the hippocampus (P < 0.01) and temporal and parietal (P < 0.05) cortices.

2014年12月4日 · Here we used JZL184, a selective inhibitor of monoacylglycerol lipase (MAGL), to examine the effects of chronic MAGL inhibition on the behavioral, biochemical, and synaptic properties of aged Ts65Dn mice, a genetic model of DS.

JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH. For research use only. We do not sell to patients. * Please select Quantity before adding items.

2013年10月25日 · JZL184 is commonly known as a highly efficacious and selective inhibitor of MAGL, a 2AG-degrading enzyme ; it has been reported that JZL184 has potent immunosuppressive and anti-inflammatory properties . We are now reporting that a single dose of JZL184 (16 mg/kg, i.p.) is able to decrease several lung inflammation parameters during the …

JZL 184 is a potent and selective MAGL inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC 50 = 8 nM). Potentiates depolarization-induced suppression of excitability in cerebellar Purkinje neurons. Exhibits >300-fold selectivity for MAGL over FAAH in vitro.

Using mouse models of advanced breast and prostate cancer and osteosarcoma, we report that the verified MAGL inhibitor JZL184 inhibited cancer-related bone damage, reduced skeletal tumour growth, suppressed cachexia and prolonged survival.