HC-030031 (TOSLAB-829227)

Description: HC-030031 (also known as TOSLAB 829227) is a novel, potent and selective blocker/antagonist/inhibitor of TRPA1 (transient receptor potential ankyrin 1) channel. It antagonizes AITC (allyl isothiocyanate)- and formalin-evoked calcium influx with IC50 of 6.2 uM and 5.3 uM respectively. As an inhibitor of TRPA1, HC-030031 can be used as a tool to study the role of TRPA1 channel in pain perception. In the FLIPR calcium-influx assay, HC-030031 blocks cinnamaldehyde- and AITC- induced activation of TRPA1 with IC50 values of 4.9uM and 7.5uM, respectively. HC-030031 is selective against TRPA1. It shows no significant inhibitory activity against many other enzymes, receptors and transporters. It also has no effect on the activation of TRPV1, TRPV3 and TRPV4.

References: Proc Natl Acad Sci U S A. 2007 Aug 14; 104(33):13525-30; Mol Pain. 2008 Oct 27; 4:48. doi: 10.1186/1744-8069-4-48; PLoS One. 2012; 7(8):e43597.