TRPM8 Antagonist |
| Katalog-Nr.GC30893 |
Der TRPM8-Antagonist ist ein potenter und selektiver TRPM8-Antagonist mit einem IC50-Wert von 0,2 nM, der in der Erforschung neuropathischer Schmerzsyndrome verwendet wird.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 259674-19-6
Sample solution is provided at 25 µL, 10mM.
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TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
TRPM8 Antagonist (Compound 14) is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes. TRPM8 Antagonist potently inhibits menthol-induced increase in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC50, 40 nM)[1].
TRPM8 Antagonist (1, 10, and 30 mg/kg, s.c.) shows a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. In addition, TRPM8 Antagonist (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice[1].
[1]. Bertamino A, et al. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018 Jul 10. doi: 10.1021/acs.jmedchem.8b00545.
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