1. Membrane Transporter/Ion Channel
  2. Chloride Channel

Chloride Channel

Chloride channels represent a relatively under-explored target class for drug discovery as elucidation of their identity and physiological roles has lagged behind that of many other drug targets. Chloride channels are involved in a wide range of biological functions, including epithelial fluid secretion, cell-volume regulation, neuroexcitation, smooth-muscle contraction and acidification of intracellular organelles. Mutations in several chloride channels cause human diseases, including cystic fibrosis, macular degeneration, myotonia, kidney stones, renal salt wasting and hyperekplexia. Chloride-channel modulators have potential applications in the treatment of some of these disorders, as well as in secretory diarrhoeas, polycystic kidney disease, osteoporosis and hypertension.

Chloride channel accessory proteins, also known as calcium-activated chloride channel regulators (CLCA proteins), are a family of transmembrane proteins that have been suggested to have a role in chloride conductance in epithelial cells.

Chloride Channel Related Products (23):

Cat. No. Product Name Effect Purity
  • HY-N0822
    Shikonin Inhibitor 99.80%
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM[1]. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor[2] and can also inhibit TNF-α and NF-κB pathway[3]. Shikonin decreases exosome secretion through the inhibition of glycolysis[4].
  • HY-12693
    R(+)-IAA-94 Inhibitor 99.70%
    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)[1][2][3].
  • HY-101012
    NPPB Inhibitor 99.83%
    NPPB is a blocker of the outwardly rectifying chloride channel (ORCC).
  • HY-100611
    CaCCinh-A01 Inhibitor 99.79%
    CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
  • HY-103371
    DCPIB Inhibitor 99.81%
    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK and inhibits TRESK, TASK1 and TASK3 (IC50s of 0.14, 0.95, 50.72 μM, respectively)[1]. DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM in CPAE cells[2].
  • HY-B1371A
    Spiperone hydrochloride Activator
    Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities[1][2][3][4][5].
  • HY-W040265
    Fenamic acid Inhibitor >98.0%
    Fenamic acid is a chloride channel blocker[1].
  • HY-B0679
    Lubiprostone Activator >98.0%
    Lubiprostone(SPI-0211;RU0211) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation.
  • HY-107212
    Selamectin Activator 99.89%
    Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM[1][2].
  • HY-18996
    Adjudin Inhibitor >98.0%
    Adjudin is an extensively studied male contraceptive with a superior mitochondria-inhibitory effect. Adjudin is also a potent Cl- channel blocker.
  • HY-B0493
    Niflumic acid Inhibitor 99.86%
    Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
  • HY-105917
    Endovion Inhibitor 99.27%
    Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor[1][2].
  • HY-B1221
    Flufenamic acid Inhibitor 99.92%
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
  • HY-16974
    Afoxolaner Inhibitor 99.53%
    Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod[1][2].
  • HY-100612
    T16Ainh-A01 Inhibitor >99.0%
    T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC)[1][2].
  • HY-B0908
    Meticrane Inhibitor 98.25%
    Meticrane is a diuretic. Meticrane inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension.
  • HY-B1494
    Picrotoxinin Inhibitor >98.0%
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors[1].
  • HY-100244
    NS1652 Inhibitor 99.89%
    NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.
  • HY-P0173A
    Chlorotoxin Inhibitor >98.0%
    Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
  • HY-103370
    Talniflumate Inhibitor >98.0%
    Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase[1]. Talniflumate is an orally active Ca2+-activated Cl- channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome[2].