BAY-390

BAY-390 is an inhibitor of transient receptor potential ankyrin 1 (TRPA1; IC₅₀s = 16 and 63 nM for the human and rat receptor, respectively).¹ It is selective for TRPA1 over a variety of receptors, ion channels, transporters, and enzymes at 10 µM but weakly inhibits estrogen receptor α (ERα), progesterone receptor B (PR-B), and the dopamine transporter (DAT; IC₅₀s = 5,000, 5,000, and 1,200 nM, respectively). BAY-390 (3-10 mg/kg) reduces the number of flinches and the duration of paw licking in a rat model of nocifensive behavior induced by the TRPA1 agonist cinnamaldehyde and reduces inflammatory pain induced by complete Freund’s adjuvant (CFA) in rats. It also reverses mechanical allodynia in a rat model of neuropathic pain induced by spinal nerve ligation when administered at a dose of 90 mg/kg twice per day.

WARNING This product is not for human or veterinary use.

1. Mesch, S., Walter, D., Laux-Biehlmann, A., et al. Discovery of BAY-390, a selective CNS penetrant chemical probe as transient receptor potential ankyrin 1 (TRPA1) antagonist. J. Med. Chem. 66(2), 1583-1600 (2023).