Description
A TRPM8 antagonist (IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor); >100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes; inhibits cold- and WS-12-induced calcium flux in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively); reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs when administered as an i.v. infusion at 46.67 μg/kg per minute; decreases the core body temperature in rats at 100 and 300 mg/kg
Formal name: 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-benzoic acid
Synonyms:
Molecular weight: 428.5
CAS: 1398583-31-7
Purity: ≥98%
Formulation: A solid
