Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade[1][2][3].
ANO1-IN-1 (Compound 9c) is a selective ANO1 channel blocker with an IC50 of 2.56 μM and 15.43 μM against ANO1 and ANO2, respectively. ANO1-IN-1 suppresses strongly proliferation of glioblastoma cells[1].
ANO1-IN-2 (Compound 10q) is a selective ANO1 channel blocker with an IC50 of 1.75 μM and 7.43 μM against ANO1 and ANO2, respectively. ANO1-IN-2 suppresses strongly proliferation of glioblastoma cells[1].
Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase[1]. Talniflumate is an orally active ca2+-activated Cl- channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome[2].
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities[1][2][3][4][5].
MONNA is a potent transmembrane protein 16A (TMEM16A,Anoctamin-1) blocker with IC50 of 80 nM. MONNA induces vasorelaxation of rodent resistance arteries in presence or absence of chloride ions[1].
DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC), voltage-dependently activates potassium channels TREK1 and TRAAK, inhibits TRESK, TASK1 and TASK3 (IC50s, 0.14, 0.95, 50.72 μM, respectively)[1]. DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM in CPAE cells[2].