| Name | JZL 184 |
| Description | JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively. |
| Cell Research | 1 × 105 cells are split into four-well chamber slides and incubated with culture medium containing BrdU for 4 h. BrdU staining is performed following the manufacturer's instructions.(Only for Reference) |
| Kinase Assay | activity-based protein profiling (ABPP): Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s |
| In vitro | JZL184 is a useful tool for studying the effects of endogenous 2-AG signaling. JZL184 displays time-dependent inhibition of MAGL and exhibits >300-fold selectivity for MAGL over FAAH in vitro. JZL184 does not interact with CB1 or CB2 receptors and does not inhibit the 2-AG biosynthetic enzymes diacylglycerol lipase-αand diacylglycerol lipase-β, or the arachidonic acid–mobilizing enzyme cytosolic phospholipase A2 group IVA. [1] |
| In vivo | JZL184 produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in eight-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL184-treated mice showed a wide array of CB1-dependent behavioral effects, including analgesia, hypomotility and hypothermia, that suggest a broad role for 2-AG–mediated endocannabinoid signaling throughout the mammalian nervous system. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 93 mg/mL (178.7 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | MAGL | neurons | inhibit | 2-Arachidonoylglycerol | JZL-184 | Inhibitor | hydrolysis | Monoacylglycerol lipase | analgesia | JZL 184 | antinociceptive |
| Inhibitors Related | Atglistatin | WWL70 | KML29 | Y-320 | ABX-1431 | URB602 | JJKK 048 | AA38-3 | Endothelial lipase inhibitor-1 | XEN445 | NG-497 | Beta-Sitosterol |
| Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Bioactive Lipid Compound Library |
United States
