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JZL 184

JZL 184
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.
Catalog No. T6554Cas No. 1101854-58-3
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Purity:97.89%
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JZL 184

Catalog No. T6554Cas No. 1101854-58-3

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.
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Pack SizePriceAvailabilityQuantity
5 mg$34In Stock
10 mg$54In Stock
25 mg$116In Stock
50 mg$219In Stock
100 mg$397In Stock
200 mg$535In Stock
1 mL x 10 mM (in DMSO)$57In Stock
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Product Introduction

Bioactivity
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.
Targets&IC50
MAGL:8 nM
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]
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
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)
AliasJZL184
Chemical Properties
Molecular Weight520.49
FormulaC27H24N2O9
Cas No.1101854-58-3
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9213 mL9.6063 mL19.2127 mL96.0633 mL
5 mM0.3843 mL1.9213 mL3.8425 mL19.2127 mL
10 mM0.1921 mL0.9606 mL1.9213 mL9.6063 mL
20 mM0.0961 mL0.4803 mL0.9606 mL4.8032 mL
50 mM0.0384 mL0.1921 mL0.3843 mL1.9213 mL
100 mM0.0192 mL0.0961 mL0.1921 mL0.9606 mL

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