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Potent and selective reversible MAGL inhibitor (IC50 = 46 nM). Exhibits 35-fold and 150-fold higher selectivity over human FAAH and ABHD6, respectively (IC50 values are 1.79 and 7.24 μM, respectively). Displays affinity for H1 receptors (pA2 = 6.81). Exhibits no activity at cannabinoid receptors at 10 μM.
|Storage||Store at +4°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 405.88. 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||2.46 mL||12.32 mL||24.64 mL|
|5 mM||0.49 mL||2.46 mL||4.93 mL|
|10 mM||0.25 mL||1.23 mL||2.46 mL|
|50 mM||0.05 mL||0.25 mL||0.49 mL|
References are publications that support the biological activity of the product.
Patel et al (2015) Loratadine analogues as MAGL inhibitors. Bioorg.Med.Chem.Lett. 25 1436 PMID: 25752982
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Keywords: JZP 361, JZP 361 supplier, Potent, selective, reversible, MAGL, inhibitors, inhibits, H1, histamine, receptors, 5851, Tocris Bioscience
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Literature in this Area
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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.