chloridechannel

Betaine chloride (Betaine hydrochloride) is an acidic form of betaine, a vitamin-like substance observed in grains and other foods; gains the amplification of DNA by decreasing the formation of secondary structure in GC-rich regions.

Urethane (Ethyl carbamate; Ethylurethane) is a byproduct formed during the fermentation process of various foods. As an ethyl ester of carbamic acid, it has the ability to inhibit the growth of bacteria, sea urchin eggs, protozoa, and plant tissues, and is commonly used for establishing lung cancer models.

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

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.

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.

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.

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.

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.

(+)-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.

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).

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).

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.

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

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

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.

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

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.

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

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.

S9-A13 is a potent and selective inhibitor of SLC26A9, exhibiting an IC50 of 90.9 nM without inhibiting other members of the SLC26 family, such as SLC26A3, SLC26A4, and SLC26A6. It also inhibits the SLC26A9 Cl- current in cells lacking CFTR expression.

ANO1-IN-4 (Compound 10bm) is a reversible inhibitor of the calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1), with an IC50 of 0.030 µM. It demonstrates good metabolic stability in rat liver microsomes and can inhibit spontaneous contractions in isolated mouse ileum.

Crofelemer (Provir) is an orally active antidiarrheal agent. It targets the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CACC), which are responsible for chloride and fluid secretion in the gastrointestinal tract. Crofelemer is applicable for research in diarrhea-related conditions.

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