A potent and selective inhibitor of MAGL that displays IC50 values of 8 nM and 4 µM for inhibition of MAGL and FAAH in mouse brain membranes

JZL 184 – 5 mg

Brand:
Cayman
CAS:
1101854-58-3
Storage:
-20
UN-No:
Non-Hazardous - /

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. JZL 184 is a potent and selective inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 8 nM and 4 µM for inhibition of MAGL and fatty acid amide hydrolase in mouse brain membranes, respectively.{16639} When administered to mice at 16 mg/kg, intraperitoneally, JZL 184 reduces MAGL activity by 85%, elevates brain 2-AG levels by 8-fold, and elicits analgesic activity in a variety of pain assays that qualitatively mimics direct central cannabinoid (CB1) agonists.{16639}  

 

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Description

A potent and selective inhibitor of MAGL that displays IC50 values of 8 nM and 4 µM for inhibition of MAGL and FAAH in mouse brain membranes, respectively

Formal name: 4-nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate

Synonyms: 

Molecular weight: 520.5

CAS: 1101854-58-3

Purity: ≥97%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Fatty Acid Metabolism||Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids||Research Area|Neuroscience|Pain Research

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