Catalog No.: PC-28382Not For Human Use, Lab Use Only.
AMG2850 is a potent and selective antagonists of TRPM8, potently inhibits menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8 with IC50 of 156 nM.
AMG2850 is a potent and selective antagonists of TRPM8, potently inhibits menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8 with IC50 of 156 nM.
AMG2850 is selective for TRPM8 relative to the recombinant TRP family members TRPA1, capsaicin activated TRPV1, 2-Aminoethoxydiphenyl borate activated TRPV3, and 4α-phorbol 12, 13-didecanoate activated TRPV4.
AMG2850 is potent in vitro at rat TRPM8 (IC90 against icilin activation of 204 ± 28 nM), highly selective (>100-fold IC90 over TRPV1 and TRPA1 channels), and orally bioavailable (F po > 40 %).
AMG2850 blocks menthol-induced action potentials but not mechanical activation in C fibers.
AMG2850 exhibits significant target coverage in vivo in a TRPM8-mediated icilin-induced wet-dog shake (WDS) model in rats (at 10 mg/kg p.o.).
