功能与背景:
A-967079 is a TRPA1 antagonist (1) and cell permeable. It has been found to be a potent blocker of TRPA1 channels. It is an oxime analogue and resembles AP18 from a structural perspective, although it has a methyl addition and a chlorine–fluorine substitution. However, compared with AP18 and HC-030031, A-967079 is significantly more potent (100-fold on human and 24-fold on rat TRPA1) and has a much improved pharmacokinetic profile. A-967079 is also more selective, with >1000-fold selectivity over other TRP channels and >150-fold selectivity over 75 other tested proteins (2).