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Potent TRPM8 antagonist (IC50 values are 0.8, 3.0 and 4.4 nM for canine, human and rat channels respectively). Exhibits antiallodynic properties in pain models in vivo.
|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 467.41. 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||2.14 mL||10.7 mL||21.39 mL|
|5 mM||0.43 mL||2.14 mL||4.28 mL|
|10 mM||0.21 mL||1.07 mL||2.14 mL|
|50 mM||0.04 mL||0.21 mL||0.43 mL|
References are publications that support the biological activity of the product.
Parks et al (2011) Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists. J.Med.Chem. 54 233 PMID: 21128593
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Keywords: TC-I 2014, TC-I 2014 supplier, TC-I2014, TRPM8, antagonist, TRPM, 5410, Tocris Bioscience
1 Citation for TC-I 2014
Citations are publications that use Tocris products. Selected citations for TC-I 2014 include:
Diver et al (2019) Structural insights into TRPM8 inhibition and desensitization. Science 365 1434 PMID: 31488702
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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.