Formulation: A solid
Formal Name: 3,6-dihydro-3′-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-[1(2H),2′-bipyridine]-4-carboxamide
Purity: ≥98%
Formula Markup: C19H15F6N3O3S
Formula Weight: 479,4
Shelf life (days): 1460
CAS Number: 824982-41-4
Notes: A-784168 is a transient receptor potential vanilloid 1 (TRPV1) competitive antagonist.{54682} 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; Item No. 90057), or anandamide (Item No. 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.{54683}