TRPM8 antagonist 14

Modify Date: 2024-01-03 21:36:43

TRPM8 antagonist 14 Structure
TRPM8 antagonist 14 structure
Common Name TRPM8 antagonist 14
CAS Number 259674-19-6 Molecular Weight 398.5
Density N/A Boiling Point N/A
Molecular Formula C26H26N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of TRPM8 antagonist 14


TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

 Names

Name TRPM8 Antagonist

 TRPM8 antagonist 14 Biological Activity

Description TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
Related Catalog
Target

IC50: 0.2 nM (TRPM8)[1]

In Vitro 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].
In Vivo 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].
Animal Admin Mice[1] Icilin, a TRPM8 agonist, is dissolved in 20% DMSO and 1% Tween 80 in distilled water and injected intraperitoneally (i.p.) in a volume of 10 mL/kg. Each animal is acclimatized for 30 min for two consecutive days before icilin administration. TRPM8 Antagonist (compound 14) stock is prepared in DMSO and diluted in saline for injections. Gabapentin is dissolved in saline and administered s.c. at the dose of 25 mg/kg 60 min prior to icillin injection. Control animals receive the vehicle injection[1].
References

[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.

 Chemical & Physical Properties

Molecular Formula C26H26N2O2
Molecular Weight 398.5
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Price: ¥2750/10 mM * 1 mL in DMSO

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