Selective CaV3.1 channel blocker (IC50 values are 0.2 and 31.8 μM for hCaV3.1 and hCaV3.2 respectively). Also reversibly inhibits NaV1.8 and blocks KV2.1 channels.
Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a 1b dimer), preferentially binds to the channel in its closed inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.