TRPM ANTAGONIST M8-AN (C15-1305-023)

General description

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.

Biochem/physiol Actions

Primary Target
TRPM8

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 400.32. Empirical Formula: C₁₈H₁₆F₄N₂O₄. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. potency: 10.9 . nM IC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.