Membrane Transporters-Ion Channels

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  1. 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.
  2. K+ (KATP) channel activator

    Y-26763 is a K+ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K+ (KATP) channel activator.
  3. Cl- transport inhibitor

    H100 is a Cl- transport inhibitor, with partial effects against both the NaK2Cl cotransporter and the Band 3 anion exchanger, but no effect against KCl cotransporter, in human erythrocytes.
  4. LY450108 is an alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor potentiator.
  5. glutamate release inhibitor

    Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke.
  6. Istaroxime hydrochloride is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).

  7. 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.
  8. P-gp modulator

    Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  9. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  10. Na+/K+ ATPase inhibitor

    Melittin is a Na+/K+ ATPase inhibitor. It inhibits Gs and stimulates Gi activity. It inhibits protein kinase C and cAMP-dependent protein kinases.
  11. 20-HETE is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells.
  12. Calcium-Sensing Receptor Antagonist

    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  13. Calcium channel blocker

    NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
  14. Sodium Channel inhibitor

    Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
  15. hERG1 potassium channel activator

    KB130015 is a novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages.
  16. TRPV1 modulator

    MRS1477 is a TRPV1 positive allosteric modulator.
  17. MCT inhibitor

    7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.
  18. 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.
  19. TRPM8 Antagonist

    AMG-333 is a potent and selective TRPM8 Antagonist.
  20. TRPC6 inhibitor

    SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
  21. L-type calcium-channel antagonist

    Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
  22. AQP7 inhibitor

    Z433927330 is a potent and selective inhibitor of Aquaporin-7 (AQP7), less potently inhibits AQP3 and AQPs9, with IC50s of ~0.2 ?M, ~0.7 ?M and ~1.1 ?M for mAQP7, mAQP3 and mAQP9, respectively.
  23. Na+/Ca2+ exchanger (NCX) inhibitor

    ORM-10103 is a specific inhibitor of the Na+/Ca2+ exchanger (NCX), which decreases the NCX current with estimated IC50s of 55 and 67 nM at -80 and at 20 mV, respectively.
  24. EAAT2 modulator

    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  25. L-Palmitoylcarnitine is a fatty acid metabolite.
  26. Cav 2.2 blocker

    Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC50 of 1 nM.
  27. TRPM8 antagonist

    TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
  28. H+/K+-ATPase inhibitor

    SCH28080 inhibits gastric H+/K+-ATPase by K+-competitive binding, with an IC50 value of 20 nM in rabbit microsomal membranes. Antisecretory and cytoprotective activities.
  29. CRAC inhibitor

    CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
  30. NecroX-5 is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.
  31. Nav1.7 inhibitor

    PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
  32. CFTR amplifier

    PTI-428 is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier.
  33. TRPC6 inhibitor

    SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
  34. HERG activator

    RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
  35. VMAT2 inhibtior

    NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM.
  36. nuclear export receptor CRM1 inhibitor

    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
  37. KCa1.1 channels activator

    NS 11021 is a potent and specific Ca2-activated big-conductance K?? Channels (KCa1.1 channels) activator.
  38. potassium current activator

    NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
  39. Potassium Channel inhibitor

    Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion.
  40. BeKm-1 is a HERG (human ether-a-go-go-related gene) blocking compound. BeKm-1 can be used for the research of heart disease.

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