A-784168

A-784168 is a transient receptor potential vanilloid 1 (TRPV1) competitive antagonist. It inhibits capsaicin-induced activation of TRPV1 in 1321N1 cells expressing TRPV1 (IC50 = 25 nM for the human receptor). A-784168 is selective for TRPV1 over a panel of 74 neurotransmitter receptors, ion channels, and other TRP channels at 50 µM but does act as an antagonist at TRP melastatin 8 (TRPM8, IC50 = 20.8 µM). It also inhibits TRPV1 activation induced by mildly acidic conditions, N-arachidonoyl dopamine (NADA, Cay-90057), or anandamide (Cay-90050) in HEK293 cells (IC50s = 14, 33.7, and 35.1 nM, respectively). It inhibits capsaicin-induced currents in primary rat dorsal root ganglion neurons (IC50 = 10 nM). A-784168 (200 µmol/kg) inhibits thermal hypersensitivity and mechanical hypersensitivity induced by NGF in rats.Formal Name: 3,6-dihydro-3'-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-[1(2H),2'-bipyridine]-4-carboxamide. CAS Number: 824982-41-4. Molecular Formula: C19H15F6N3O3S. Formula Weight: 479.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 40 mg/ml. SMILES: O=C(C1=CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=CC=C(S(=O)(C(F)(F)F)=O)C=C3. InChi Code: InChI=1S/C19H15F6N3O3S/c20-18(21,22)15-2-1-9-26-16(15)28-10-7-12(8-11-28)17(29)27-13-3-5-14(6-4-13)32(30,31)19(23,24)25/h1-7,9H,8,10-11H2,(H,27,29). InChi Key: SDUAWRFBHRAFBM-UHFFFAOYSA-N.