A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and it also causes elevation of arterial blood pressure and an elevation
TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR, and RET with IC50s of 10 nM, 4.8 nM, 600 nM, and 29 nM, respectively) in a panel of 192 kinases.
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.