Mambalgin 1 TFA is a potent and selective inhibitor of ASIC1a. It exhibits IC50 values of 192 nM for human ASIC1a and 72 nM for ASIC1a/1b dimer, binding to closed/inactive channels. This compound demonstrates high selectivity for ASIC1a over a range of other channels including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. Research indicates its ability to increase the latency of withdrawal response in mouse tail-flick and paw-flick tests.
- Selective ASIC1a inhibitor
- Binds to closed/inactive channels
- Increases latency of withdrawal response in mouse tail-flick and paw-flick tests