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  • Membrane Transporters-Ion Channels

Membrane Transporters-Ion Channels

Items 1-50 of 2532

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  1. A10758
    PTC124 (Ataluren)

    CFTR inhibitor

    PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.
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  2. A13344
    Pico145

    TRPC1/4/5 channels inhibitor

    Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
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  3. A13647
    (-)-Blebbistcitin

    myosin II inhibitor

    Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
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  4. A11750
    Ibutilide fumarate
    Ibutilide is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm. It exerts its antiarrhythmic effect by induction of slow inward sodium current, which prolongs action potential and refractory period (physiology) of myocardial cells.
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  5. A16993
    Quinine

    Antimalarial

    Quinine is a primary alkaloid of various species of Cinchona, optical isomer of Quinidine and an anti-malarial, skeletal, muscle relaxant.
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  6. A12519
    VX-661

    CFTR corrector

    VX-661 is another cystic fibrosis transmembrane conductance regulator (CFTR) corrector in development for the treatment of cystic fibrosis.
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  7. A10985
    VX-770 (Ivacaftor)

    CFTR activator

    VX-770 (Ivacaftor) is known as a CFTR potentiator.
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  8. A15810
    7ACC1

    MCT Inhibitor?€?

    7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
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  9. A12755
    Ouabain

    a-K-ATPase inhibitor

    Ouabain is a selective Na+, K+-ATPase inhibitor.
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  10. A10986
    VX-809 (Lumacaftor)

    CFTR modulator

    VX-809 is the second investigational oral candidate compound for the treatment of cystic fibrosis (CF).
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  11. A12897
    CFTRinh-172

    CFTR inhibitor

    CFTRinh-172 is a voltage-independent, selective CFTR inhibitor
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  12. A13723
    CFTR-Inhibitor-II

    CFTR inhibitor

    CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).
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  13. A10487
    Isradipine

    calcium channel blocker

    Isradipine is a calcium channel blocker of the dihydropyridine class.
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  14. A15865
    RSL3

    Ferroptosis inhibitor

    RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
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  15. A14242
    Digoxin

    sodium-potassium pump inhibitor

    Digoxin is a sodium-potassium pump inhibitor.
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  16. A16398
    Ambroxol HCl

    Sodium Channel inhibitor

    AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
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  17. A13109
    NBQX (FG9202)

    AMPA Receptor Antagonist

    NBQX is a potent, selective and competitive AMPA receptor antagonist.
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  18. A11206
    CK-1827452 (Omecamtiv mecarbil)

    Myosin activator

    CK-1827452 is a selective cardiac specific myosin activator.
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  19. A10179
    Carbamazepine
    Carbamazepine is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia.
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  20. A15275
    Vernakalant HCl

    Ion channel blocker

    Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
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  21. A20445
    Nanvuranlat (JPH203)

    LAT-1 inhibitor

    JPH203 is a potent and selective L-type amino acid transporter 1 (LAT-1) inhibitor.
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  22. A10213
    Ciclopirox
    Ciclopirox is currently being investigated as an alternative treatment to ketoconazole for seborrhoeic dermatitis as it suppresses growth of the yeast Malassezia furfur.It acts by inhibiting the membrane transfer system by interrupting the Na+ K+ ATPase.
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  23. A20786
    Pyr10

    TRPC3 inhibitor

    Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.
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  24. A18426
    ML418

    Kir7.1 potassium channels blocker

    ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
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  25. A12353
    A 967079

    TRPA1 channel blocker

    A 967079 is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively).
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  26. A10549
    LY335979 (Zosuquidar 3HCl)

    P-gp modulator

    LY335979 (Zosuquidar trihydrochloride) is a potent highly selective P-gp inhibitor.
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  27. A12324
    Elacridar (GF120918)

    P-gp & BCRP inhibitor

    Elacridaris a prototypical BCRP inhibitor which inhibits the Bcrp1-mediated transport.
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  28. A14186
    AZD-3965

    MCT1 inhibitor

    AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.
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  29. A13822
    Erastin

    VDAC inhibitor

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
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  30. A14023
    BAPTA/AM

    Selective calcium chelator

    BAPTA/AM, an intracellular calcium chelator, induces delayed necrosis by lipoxygenase-mediated free radicals in mouse cortical cultures.
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  31. A11584
    Tariquidar (XR9576)

    P-gp inhibitor

    Tariquidar (XR9576) is a P-glycoprotein drug efflux pump inhibitor.
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  32. A12349
    Ampalex (CX-516)
    Ampalex is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator
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  33. A11293
    AR-C155858

    MCT1 and MCT2 inhibitor

    AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.
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  34. A10554
    Manidipine 2HCl
    Manidipine 2HCl is a HCl salt form of Manidipine which is a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.
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  35. A11961
    Bafilomycin A1

    ATPase inhibitor

    Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells.
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  36. A13900
    Disopyramide

    Sodium channel blocker

    Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.
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  37. A11521
    PAP-1 (5-(4-Phenoxybutoxy)psoralen)

    Kv1.3 blocker

    PAP-1 is a selective inhibitor of Kv1.3, voltage-gated potassium channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity.
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  38. A12783
    TRAM-34

    Potassium Channel Blocker

    TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.
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  39. A10645
    Nimodipine

    Calcium Channel inhibitor

    Nimodipine is a L-type Ca2+ channel blocker.
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  40. A20092
    EIPA

    TRPP3 channel inhibitor

    EIPA (L593754; MH 12-43) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA (L593754; MH 12-43) also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
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  41. A16103
    GsMTx4

    MSCs Inhibitor

    GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.
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  42. A11080
    PSC-833 (Valspodar)

    MDR1/P-gp Inhibitor

    PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
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  43. A10723
    Phloretin (Dihydronaringenin)
    Phloretin inhibits the active transport of glucose into cells by SGLT1 and SGLT2, though the inhibition is weaker than by its glycoside phlorizin.
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  44. A10724
    Phlorizin (Phloridzin)

    SGLT1/SGLT2 inhibitor

    Phlorizin is a competitive inhibitor of SGLT1 and SGLT2; this reduces renal glucose transport, lowering the amount of glucose in the blood.
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  45. A10669
    Oligomycin A

    ATPase inhibitor

    Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.
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  46. A14011
    Tenapanor

    NHE3 inhibitor

    Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.
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  47. A12727
    AMG517

    TRPV1 antagonist

    AMG 517 is a potent and selective TRPV1 antagonist.
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  48. A13372
    CHC

    MCT inhibitor

    CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.
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  49. A10285
    Dapagliflozin (BMS512148)

    SGLT2 inhibitor

    Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.
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  50. A20954
    Minocycline hydrochloride

    HIF-1α inhibitor

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
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  6. Blocker 99items
  7. Inducer 3items
  8. Potentiator 6items
  9. Ligand 2items