AMG 2850

AMG 2850 is an antagonist of transient receptor potential melastatin 8 (TRPM8). It inhibits menthol- or cold-induced intracellular calcium release in CHO cells expressing rat TRPM8 (IC50s = 7. and 150 nM, respectively). AMG 2850 is selective for TRPM8 over transient receptor potential ankyrin 1 (TRPA1), transient receptor potential vanilloid 1 (TRPV1), TRPV3, and TRPV4 (IC50s = >20, >10, >10, and >10 µM, respectively). In vivo, AMG 2850 (100 mg/kg) decreases body temperature in rats and mice. It also inhibits wet-dog shakes induced by icilin (Cay-10137) in rats when administered at a dose of 10 mg/kg.. Solulibility: DMSO: Soluble: =10 mg/ml: Ethanol: Soluble: =10 mg/ml.