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OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation.
TMinh-23 is (Compound 10bm) is a potent, selective inhibitor of transmembrane protein 16A (TMEM16A or ANO1, DOG1, ORAOV2, TAOS-2) with IC50 of 30 nM in short-circuit current assays, weakly inhibits TMEM16B (IC50=400 nM, 13 -fold selectivity).
1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).
OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation.
CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and no off-target engagement a diverse panel of 61 CNS receptors, channels, and transporters expressed in brain tissue.AK-42 binds to an extracellular vestibule above the channel pore. AK-42 is almost three orders-of-magnitude more potent than MCFA, demonstrates high potency (IC50=14 nM for rat CLC-2) in manual patch-clamp experiments on CHO cells transiently transfected with rat CLC-2.AK-42 inhibits hyperpolarization-activated current in hippocampal cells, attenuates steady-state currents and eliminated relaxation currents in recorded neurons.AK-42 is a powerful tool for investigating CLC-2 neurophysiology.
DRAinh-A250 is a specific inhibitor of Cl-/anion exchanger SLC26A3 (DRA), fully and reversibly inhibits SLC26A3-mediated Cl- exchange with HCO3-, I-, and thiocyanate (SCN-) with IC50 of ~0.2 uM.
CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport i
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