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Potent and selective TRPM8 antagonist (IC50 values are 13 and 20 nM for hTRPM8 and rTRPM8, respectively). Displays high selectivity over other TRP channels (IC50 >20 μM, TRPV1/V3/V4/A1). Inhibits icilin-induced wet-dog shake in rats and suppresses cold-induced increases in blood pressure in the rat cold-pressor test.
|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 453.33. 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||2.21 mL||11.03 mL||22.06 mL|
|5 mM||0.44 mL||2.21 mL||4.41 mL|
|10 mM||0.22 mL||1.1 mL||2.21 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Horne et al (2018) Discovery of TRPM8 antagonist (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid (AMG 333), a clinical candidate for the treatment of migraine. J.Med.Chem. 61 8186 PMID: 30148953
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Keywords: AMG 333, AMG 333 supplier, AMG333, Potent, selective, TRPM8, antagonists, antagonism, transient-receptor-potential, melastatin, 8, cold-temperature, thermosensor, TRPM, 6874, Tocris Bioscience
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Literature in this Area
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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.