JZL184

SKU: orb1222875

Description

JZL184 is highly selective, and potent MAGL inhibitor ( monoacylglycerol lipase inhibitor). JZL184 improves behavior and neural properties in Ts65Dn mice, a model of down syndrome. JZL184 attenuates LPS-induced increases in cytokine expression in the rat frontal cortex and plasma: differential mechanisms of action. JZL184 also suppresses inflammatory pain in the mouse carrageenan model.

Key Properties

• CAS Number: 1101854-58-3
• MW: 520.49
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₄N₂O₉
• SMILES: OC(C1CCN(CC1)C(=O)Oc1ccc(cc1)[N+](=O)[O-])(c1ccc2OCOc2c1)c1ccc2OCOc2c1
• Target: MAGL
• Solubility: DMSO : ≥ 35 mg/mL; 67.24 mM

Bioactivity

• In Vivo:
  JZL 184 (4-40 mg/kg; intraperitoneal injection; once; C57Bl/6 mice) treatment produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL 184-treated mice shows a remarkable array of CB1-dependent behavioral effects, including analgesia, hypomotility, and hypothermia. JZL 184 prolongs depolarization-induced suppression of excitation (DSE) in Purkinje neurons in cerebellar slices and DSE inhibition (DSI) in CA1 pyramidal neurons in hippocampal slices. JZL 184 produces greater enhancement of DSE/DSI in mouse neurons than that in rat neurons. Animal model: Male C57Bl/6 mice (6-8 weeks old, 20-26 g). Dosage: 4 mg/kg, 8 mg/kg, 16 mg/kg, 40 mg/kg. Administration: Intraperitoneal injection; once. Result: Produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that were maintained for at least 8 h.
• In Vitro:
  JZL 184 displays IC50 values of 8 nM and 4 μM for blockade of 2-AG and oleamide (FAAH substrate) hydrolysis in brain membranes, respectively. Comparable inhibitory effects are observed with recombinant MAGL and FAAH when expressed in COS7 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JZL184 | JZL 184 | JZL-184

Quick Database Links

Gene Symbol

MAGL