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JZL 184

Catalog No. T6554 CAS 1101854-58-3

Synonyms: JZL184

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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JZL 184, CAS 1101854-58-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 34.00
10 mg	In stock	$ 54.00
25 mg	In stock	$ 116.00
50 mg	In stock	$ 219.00
100 mg	In stock	$ 397.00
200 mg	In stock	$ 535.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 97.89%

Purity: 97.6%

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Storage & Solubility Information

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)

Synonyms	JZL184
Molecular Weight	520.49
Formula	C27H24N2O9
CAS No.	1101854-58-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

References and Literature

1. Long JZ, et al. Nat Chem Biol, 2009, 5(1), 37-44. 2. Ye L, et al. Cancer Lett, 2011, 307(1), 6-17.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Anti-Metabolism Disease Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library Target-Focused Phenotypic Screening Library Bioactive Lipid Compound Library Metabolism Compound Library Lipid Metabolism Compound Library

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Keywords

JZL 184 1101854-58-3 Metabolism Lipase MAGL neurons inhibit 2-Arachidonoylglycerol JZL-184 Inhibitor hydrolysis JZL184 Monoacylglycerol lipase analgesia antinociceptive inhibitor

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