JZL-184

SKU: orb1300664

Description

JZL 184 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor, exhibiting an IC50 of 8 nM for MAGL versus 4 µM for FAAH. This tool compound is widely used in neuroscience research to study endocannabinoid signaling in both in vitro assays and in vivo models.

Research Area

Neuroscience

Key Properties

• CAS Number: 1101854-58-3
• MW: 520.50
• Purity: >98%
• Formula: C₂₇H₂₄N₂O₉
• SMILES: OC(C1CCN(CC1)C(=O)Oc1ccc(cc1)[N+]([O-])=O)(c1ccc2OCOc2c1)c1ccc2OCOc2c1
• Target: Lipase
• Solubility: Soluble in DMSO (up to 25 mg/ml).

Bioactivity

• Target IC50:
  MAGL:8 nM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MAGL, hydrolysis, Inhibitor, neurons, JZL 184, JZL184, JZL-184, Monoacylglycerol lipase, inhibit, analgesia, antinociceptive, 2-Arachidonoylglycerol

Compound Identifiers

PubChem CID

25021165