Chloride channel

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.

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).

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.

R(+)-IAA-94 (R(+)-Methylindazone) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-IAA-94 inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).

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.

Hypotaurine (2-Aminoethanesulfinic acid), functioning as an intermediate in the biosynthesis of taurine from cysteine within astrocytes, acts as an endogenous inhibitory amino acid targeting the glycine receptor.

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

Isodeoxycholic Acid is a bile acid that is formed via epimerization of deoxycholic acid by intestinal bacteria. It has a greater critical micelle concentration than DCA, indicating reduced detergent activity, and is less active than DCA in inhibiting growth in a panel of seven gut commensal bacteria species. Isodeoxycholic Acid(0.1%) inhibits spore germination induced by taurocholic acid in several C. difficile strains, as well as decreases the cytotoxicity of C. difficile culture supernatants to Vero cells. Plasma levels of isodeoxycholic acid are decreased in a rat model of high-fat diet-induced obesity compared with rats fed a normal diet.

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

Ani9 is a high selective blocker of Anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A) with an IC50 of 77 nM and can be used in studies about ANO1 and the treatment of ancer, hypertension, pain, diarrhea and asthma.

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.

ANO1-IN-1, a selective ANO1 channel blocker, inhibited ANO1 and ANO2 with IC50 values of 2.56 μM and 15.43 μM, respectively.ANO1-IN-1 had a significant inhibitory effect on the proliferation of glioma cells.

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.

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.

Eact is a selective and potent TMEM16A activator that directly activates the TRPV1 channels in sensory nociceptors, thereby producing itch, acute nociception, and thermal hypersensitivity (brackets).

Guanidinoethyl sulfonate (Taurocyamine) is a competitive glycine receptor antagonist.

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.

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

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

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

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

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.

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

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

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

Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.