GSK2193874

GSK2193874 is a potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC50 values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively. It is selective for TRPV4 over ~200 other human receptors, channels, and enzymes. GSK2193874 is effective in vivo, as it resolves pulmonary edema resulting from myocardial infarction in mice. TRPV4 blockade with GSK2193874 does not alter heart rate or blood pressure in rats, although it attenuates decreases in pulmonary and systemic arterial pressures induced by TRPV4 agonists.Formal Name: 3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide. CAS Number: 1336960-13-4. Molecular Formula: C37H38BrF3N4O. Formula Weight: 691.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 14 mg/ml, Ethanol: 15 mg/ml, Ethanol:PBS (pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 209, 241, 330 nm. SMILES: BrC1=CC=C(C(C(NC2(CC2)C3=CC=CC=C3)=O)=C(CN4CCC(N5CCCCC5)CC4)C(C6=CC=CC(C(F)(F)F)=C6)=N7)C7=C1. InChi Code: InChI=1S/C37H38BrF3N4O/c38-28-12-13-30-32(23-28)42-34(25-8-7-11-27(22-25)37(39,40)41)31(24-44-20-14-29(15-21-44)45-18-5-2-6-19-45)33(30)35(46)43-36(16-17-36)26-9-3-1-4-10-26/h1,3-4,7-13,22-23,29H,2,5-6,14-21,24H2,(H,43,46). InChi Key: UIVOZBSCHXCGPS-UHFFFAOYSA-N.