In cells

Use at concentration of 1 µM. In rat DRG neurons A-079 (1µM) reversibly blocked AITC (100 µM) responses, in accordance with a noncovalent interaction between A-079 and TRPA1 . A-079 (5 µM) reversibly blocked CGRP-release evoked by 200 µM AITC or 10 µM bradykinin, as determined by FLIPR.

We recommend to use the TRPA1 inhibitor BAY-390 also available from SGC for control experiments.

Use the recommended concentration to avoid off-target toxicity and/or off-target activity. Using concentrations that are higher than recommended could lead to false positive or confounding results.

In vivo

Oral dosing of A-079 dose dependently attenuated the nocifensive flinching evoked by 5% mustard oil relative to vehicle. A-079 had no effects on locomotor activity at these doses. In the MIA-induced osteoarthritic pain model, A-079 reversed the grip force deficit relative to vehicle with a ED₅₀ of 23.2 mg/kg, p.o.
In rat DRG neurons A-079 (1µM) reversibly blocked AITC (100 µM) responses, in accordance with a noncovalent interaction between A-079 and TRPA1 . A-079 (5 µM) reversibly blocked CGRP-release evoked by 200 µM AITC or 10 µM bradykinin, as determined by FLIPR.