Potent and selective irreversible MAGL inhibitor (IC50 values are 0.25 and 7.4 nM at rMAGL and hMAGL, respectively). Exhibits 389-fold selectivity over hFAAH and exhibits minimal binding at CB receptors (IC50 > 10 μM). Alleviates symptoms in a MS in vivo model. Exhibits analgesic effects in an acute inflammatory pain model in vivo. Ameliorates neuropathic hypersensitivity induced by oxaliplatin (Cat. No. 2623). Displays high membrane permeability and brain penetrant.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 463.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.16 mL||10.79 mL||21.58 mL|
|5 mM||0.43 mL||2.16 mL||4.32 mL|
|10 mM||0.22 mL||1.08 mL||2.16 mL|
|50 mM||0.04 mL||0.22 mL||0.43 mL|
References are publications that support the products' biological activity.
Brindisi et al (20106) Development and pharmacological characterization of selective blockers of 2-arachidonoyl glycerol degradation with efficacy in rodent models of multiple sclerosis and pain. J.Med.Chem. 59 2612 PMID: 26888301
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