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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|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 the degree 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 biological activity of the product.
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.