cl? channels

Ecabapide (DQ-2511) is a novel gastrointestinal motility promoter that significantly enhances gastric emptying in SHRSP.Ecabapide activates cyclic GMP-dependent housekeeping Cl- channels in rabbit gastric wall cells.

Selamectin (UK-124114) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg/ml) shows the effect of growth inhibition.

T16Ainh-A01 is a potent inhibitor of TMEM16A Chloride channel, inhibiting TMEM16A-mediated chloride currents (IC50 of 1 µM),and functions as a calcium-activated chloride channel (CaCC).

Niflumic acid (Nifluril) is a Ca2+-activated Cl- channel blocker and an analgesic and anti-inflammatory agent used in the therapy of rheumatoid arthritis.

Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.

Fenamic acid (N-Phenylanthranilic acid) is a chloride channel blocker that causes renal papillary necrosis in rats. Fenamic acid serves as a parent structure for several nonsteroidal anti-inflammatory drugs (NSAIDs), including flufenamic acid, tolfenamic acid, mefenamic acid, and meclofenamic acid.

Gap19 TFA is a selective and potent blocker of connexin 43 (Cx43) hemichannels, originating from nine amino acids within the Cx43 cytoplasmic loop (CL). It operates by hindering intramolecular interactions between the C-terminus (CT) and the CL, effectively inhibiting hemichannel activity without affecting GJ channels or Cx40/pannexin-1 hemichannels. This peptide offers protective benefits for the myocardium.

Lubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

CaCCinh-A01 is an inhibitor of the calcium-activated chloride channel (CaCC, 10 μM) and TMEM16A (IC50: 2.1 μM).

Eact is a selective and potent TMEM16A activator. It directly activates the TRPV1 channels in sensory nociceptors. Which also produces itch, acute nociception and thermal hypersensitivity.

Endovion (NS3728) is a pharmacological anion channel and an Anoctamin-1 (ANO 1) channel inhibitor. Endovion is also the specific VRAC/VSOAC blocker.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.

VU 0240551 is a selective antagonist of neuronal K-Cl cotransporter KCC2 inhibitor with an IC50 of 560 nM. VU 0240551 inhibits L-type calcium channels and hERG.

Irisolidone is a potent volume-regulated anion channel (VRAC) current inhibitor, it exhibits high efficacy for VRAC blockade with IC50s of 5-13 μM.

Talniflumate (Somalgen) is a calcium-activated chloride channel (hCLCA1/mCLCA3) blocker that reduces mucin synthesis and releases in animal models and cell culture. It possesses anti-inflammatory actions via inhibition of Cox (cyclooxygenase) and inhibits Cl-/HCO3- exchange activity. It also increases survival in a cystic fibrosis mouse model of the distal intestinal obstructive syndrome.

NPPB is a chloride channel blocker with IC50 of 80 nM .

Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

In epididymal epithelial cells, AF-2785 inhibits cystic fibrosis transmembrane conductance regulator Cl(-) channels.

Meticrane (Arresten) is a sulphonamide-derivative with thiazide-like diuretic activity.

MONNA is a potent TMEM16A (Anoctamin-1) blocker (IC50 : 80 nM). It induces vasorelaxation of rodent resistance arteries in presence or absence of chloride ions.

Adjudin (AF-2364) is a small molecule compound known to possess antispermatogenic function, attenuates microglia activation by suppression of the NF-κB pathway.

NS1652 is an anion conductance inhibitor. NS1652 blocks chloride channel has an IC50 of 1.6 μM in human and mouse red blood cells.