5.30617

TRPM Antagonist, M8-An

• Synonim(y): TRPM Antagonist, M8-An, TRPM8 Antagonist
• Wzór empiryczny (zapis Hilla): C₁₈H₁₆F₄N₂O₄
• Masa cząsteczkowa: 400.32
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Formularz: solid
• siła działania: 10.9 nM IC₅₀
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 100 mg/mL
• temp. przechowywania: 2-8°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Primary Target
TRPM8

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable