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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; does not inhibit the homologous anion exchangers SLC26A4 (pendrin) or SLC26A6 (PAT-1), as well as other related proteins or intestinal ion channels; blocked fluid absorption in closed colonic loops but not in jejunal loops in mice, while the NHE3 (SLC9A3) inhibitor tenapanor blocked absorption only in the jejunum; reduces signs of constipation in loperamide-treated mice after oral treatment.




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 in neurons, rescues KCC2 plasma membrane expression; renormalizes stimulus-evoked responses in spinal nociceptive pathways in a rat model of neuropathic pain.



552309-42-9 T16Ainh-A01 is an inhibitor of the calcium-activated chloride channel TMEM16A, inhibits Ca2+-activated Cl− channel (CACC) activity in TMEM16A-transfected FRT cells with IC50 of 1 uM; T16Ainh-A01 (1-30 uM) inhibited single calcium (Ca2+)-activated chloride (Cl−) channels and whole cell currents activated by 500 nM free Ca2+; T16Ainh-A01 relaxed mouse thoracic aorta pre-contracted with methoxamine with an IC50 of 1.6 uM and suppressed the methoxamine concentration-effect curve; blocks calcium-activated chloride channels in vascular smooth muscle cells and relaxes murine and human blood vessels.


1181083-81-7 CLP290 (CLP-290) is an orally acirtve small molecule K+-Cl- cotransporter isotype 2 (KCC2) activator, the carbamate prodrug of CLP257; In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons. Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior.


54197-31-8 IAA-94 is an indanyloxyacetic acid (IAA) inhibitor of epithelial chloride channels that binds channels in bovine kidney cortex microsomes with Ki of 1 uM; significantly suppresses IGF-I-induced VSMC proliferation, also blocks cell swelling evoked glutamate release from primary microglia and MLS-9 cells; effectively reduces IFNgamma-induced NO production in microglial BV2 cells.


5970-15-0 OADS is a specific, reversible, small-molecule inhibitor directs against CLC (Chloride Channel) antiporter with Ki of 29 uM, has no specific effect on a CLC channel (ClC-1).

VU 0240551

893990-34-6 VU 0240551 is a potent, selecticve inhibitor of the neuronal K-Cl cotransporter KCC2 with IC50 of 568 nM in K+ uptake assay in KCC2-overexpressing cells; displays >100-fold selectivity over NKCCl; also shows significant inhibition (>50% at 50 µM) of several GPCRs and key ion channels (hERG and L-Type Ca2+ channels).

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