PF-05105679

PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8, IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor). It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 µg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.Formal Name: 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-benzoic acid. CAS Number: 1398583-31-7. Molecular Formula: C26H21FN2O3. Formula Weight: 428.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 10 mg/ml. lambdamax: 232 nm. SMILES: O=C(N([C@@H](C1=CC=C(F)C=C1)C)CC2=CC=CC(C(O)=O)=C2)C3=CC4=C(C=CC=C4)N=C3. InChi Code: InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1. InChi Key: BXNMZRPTQFVRFA-QGZVFWFLSA-N.