J3455 Sigma

JZL 184 hydrate

≥98% (HPLC)

Synonym: JZL184 hydrate

  • Empirical Formula (Hill Notation) C27H24N2O9 · xH2O

  • Molecular Weight 520.49 (anhydrous basis)

  •  MDL number MFCD12912421

Properties

Related Categories Cancer Metabolism, Cancer Research, Cannabinoids, Cell Biology, Cell Signaling and Neuroscience,
assay   ≥98% (HPLC)
form   powder
storage condition   desiccated
color   light yellow
solubility   DMSO: >20 mg/mL
storage temp.   2-8°C

Description

Biochem/physiol Actions

JZL184 selectively inhibits MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be the enzyme primarily responsible for the degradation of 2-AG. It is difficult to separate the activities of the two because most currently available inhibitors of MAGL are not selective, and also inhibit FAAH or other enzymes. JZL 184 is the first selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity for MAGL vs FAAH. When administered to mice, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.

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