Cravatt Reagent

SKU: orb1220772

Description

Cravatt Reagent is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

Key Properties

• CAS Number: 1438416-21-7
• MW: 462.3
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₁Cl₂N₃O₄?
• SMILES: Clc1ccc(cc1)C(N1CCN(CC1)C(=O)ON1C(=O)CCC1=O)c1ccc(Cl)cc1
• Target: Lipase
• Solubility: In Vitro: DMSO : 250 mg/mL (540.74 mM)

Bioactivity

• In Vivo:
  MJN110 (i.p.; 0.0818 mg/kg; twice daily for 5.5 days) reverses chronic constriction injury (CCI)-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner. The respective ED50 value (95% confidence limits) is 0.430 (0.233-0.793) mg/kg. Animal model: Male C57BL/6J mice ranged from 18 to 35 g. Dosage: 0.0818 mg/kg. Administration: i.p.; twice daily for 5.5 days. Result: Reversed CCI-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner.
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• In Vitro:
  MJN110 (0.01-1000 nM; 4 hours) has the primary serine hydrolase target, hMAGL, with an IC50 of ~1 nM and 10- and 100-fold selectivity windows over ABHD6 and LYPLA1/2, respectively. Western blot analysis. Cell line: Human-derived PC3 cells. Concentration: 0.01, 0.1, 1, 10, 100, 1000 nM Incubation time: 4 hours. Result: HMAGL acted as the primary serine hydrolase target with an IC50 of ~1 nM.
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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

MJN110

Quick Database Links

Gene Symbol

Lipase