Chloride channel

<p>Halothane (Anestan) 可以减弱内皮依赖性舒张作用。</p>

<p>Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties.</p>

<p>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</p>

<p>Eact is a potent TMEM16A activator that also triggers TRPV1, causing itch, pain, and heat sensitivity.</p>

<p>Meticrane (Arresten) is a sulphonamide-derivative with thiazide-like diuretic activity.</p>

<p>T16Ainh-A01 is a potent TMEM16A chloride channel inhibitor with a 1 μM IC50, targeting CaCC.</p>

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

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

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

<p>Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs.</p>

<p>High-affinity ClC-2 blocker (KD ~50 pM), selective over other ClCs/CFTR/GABAC/CaCC/KV1.2; slows activation, no effect on open channels.</p>

<p>Chlorotoxin: 36-amino acid peptide from deathstalker scorpion venom; blocks small chloride channels.</p>

<p>Chlorotoxin TFA, a scorpion venom peptide, blocks chloride channels and has anti-cancer properties.</p>

<p>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.</p>

<p>Chlorotoxin(linear): 36-amino-acid peptide from Egyptian scorpion venom, used in research as chloride channel blocker.</p>

<p>A unique collection of 931 compounds targeting ion channels for research in ion channels-related diseases and ion channel drug discovery;</p>

<p>Lubiprostone (hemiketal) (RU-0211 (hemiketal)), a selective activator of the chloride channel 2 (CLCN2), facilitates the treatment of chronic idiopathic constipation and opioid-induced constipation. It functions by enhancing CLCN2 channel activity, which boosts chloride ion secretion in the intestines, subsequently increasing fluid secretion and improving intestinal peristalsis. Additionally, Lubiprostone (hemiketal) may be utilized in research related to chronic constipation and cancer.</p>

<p>NPPB is a chloride channel blocker with IC50 of 80 nM .</p>

<p>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.</p>

<p>Guanidinoethyl sulfonate (Taurocyamine) is a competitive glycine receptor antagonist.</p>

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

<p>Anthracene-9-carboxylic acid is an inhibitor of chloride transport with a moderate to strong inhibitory action on PKA activated cardiac IcI.</p>

<p>Phenyl benzoate is a benzoate ester obtained by the formal condensation of phenol with benzoic acid.It is an important organic synthesis intermediate.</p>

<p>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.</p>

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

<p>Selamectin (UK-124114) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in</p>

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

<p>Fenamic acid (N-Phenylanthranilic acid) is a chloride channel blocker that causes renal papillary necrosis in rats.</p>

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

<p>Talniflumate (Somalgen) is a calcium-activated chloride channel (hCLCA1/mCLCA3) blocker that reduces mucin synthesis and releases in animal models and cell</p>

<p>NS5818 inhibits ClC.</p>

<p>Alilusem is a new diuretic that is beneficial to the clinical treatment of hypertension.</p>

<p>H100 inhibits Cl- transport, mildly affects NaK2Cl cotransporter and Band 3 anion exchanger, not KCl cotransporter.</p>

<p>ANO1-IN-2: potent ANO1 blocker (IC50: 1.75 μM), less effective on ANO2 (IC50: 7.43 μM), inhibits glioblastoma cell growth.</p>

<p>BTG-1640 is used potentially for the treatment of anxiety and panic disorder.</p>

<p>Bts 39542 is a diuretic that plays a major role in the Henle circulation and increases renal blood flow without affecting glomerular filtration rate.</p>

<p>IAA-94 is an inhibitor of chloride channels, it binds channels in bovine kidney cortex microsomes with a Ki value of 1 µM.</p>

<p>Hydroflumethiazide is a thiazide diuretic. It has also shown the activity of anti-hypertensive.</p>

<p>Losigamone (AO-33) is an agonist of GABA receptor and can be used in studies about the treatment of partial seizures.</p>

<p>R(+)-IAA-94 (Methylindazone) blocks epithelial chloride channels; inhibits Nef-sdAb19 binding.</p>

<p>Stepronin (TTPG) shows expectorant activities and inhibits airway secretion.</p>

<p>ANO1-IN-1 blocks ANO1/2 channels (IC50: 2.56/15.43 μM) and hinders glioma cell growth.</p>

<p>Ani9 selectively blocks ANO1/TMEM16A with a 77 nM IC50, useful for ANO1 research and treating cancer, hypertension, pain, diarrhea, asthma.</p>

<p>ARN 11391 enhances the function of the IP3-gated calcium channel ITPR1 (Inositol 1,4,5-trisphosphate (IP3) receptor type 1), boosting intracellular calcium ion</p>

<p>OADS is an inhibitor of ClC-ec1 with low micromolar affinity. OADS has no specific effect on a CLC channel (ClC-1).</p>

<p>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.</p>

<p>NMD670 is an orally active, partial inhibitor of the skeletal muscle-specific chloride channel ClC-1. It enhances muscle excitability and neuromuscular transmission, restoring muscle function and mobility. NMD670 has a favorable safety profile and improves muscle function in rats, particularly in an MG rat model [1].</p>

<p>DFBTA inhibits ANO1 with IC50 of 24 nM, effectively treating inflammatory pain orally.</p>

<p>T16A(inh)-C01 is the Ca(2+)-activated Cl(-) Channel, Ano1 class C inhibitor.</p>