TRPM Antagonist, M8-An-Calbiochem

C₁₈H₁₆F₄N₂O₄

400.32

A cell-permeable, readily bioavailable 2-picolinamide derivative that acts as a highly potent antagonist of transient receptor potential cation channel subfamily M member 8 (TRPM8; IC₅₀ = 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells stably expressing human TRPM8). At much higher levels it is shown to activate human TRPA1 (EC₅₀ = 2.8 µM) and inhibit human TRPV1 (IC₅₀ = 3.0 µM). Selectively reduces behavioral and neural responses to cooling in spinal ligated rats (~ 30 mg/kg), but not in naïve rats.
A cell-permeable, readily bioavailable 2-picolinamide derivative that acts as a highly potent antagonist of transient receptor potential cation channel subfamily M member 8 (TRPM8; IC₅₀ = 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells stably expressing human TRPM8). At much higher levels it is shown to activate human TRPA1 (EC₅₀ = 2.8 µM) and inhibit human TRPV1 (IC₅₀ = 3.0 µM). Selectively reduces behavioral and neural responses to cooling in spinal ligated rats (~ 30 mg/kg), but not in naïve rats.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Primary Target
TRPM8
Reversible: yes

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Patel, R., et al. 2014. J. Pharm. Exp. Ther.345, in press.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥98% (HPLC)

solid

10.9 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 100 mg/mL

2-8℃

Packaged under inert gas

11 - Combustible Solids

WGK 3