Membrane Transporters-Ion Channels

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  1. K+/Na+/Ca+ Channel Blocker

    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
  2. Ca2+ signaling modulator

    Astragaloside A is a novel regulator of HIF-1α and angiogenesis through the PI3K/Akt pathway in HUVECs that are exposed to hypoxia.
  3. ATPase antagonist

    PF 3716556 is H+,K+-ATPase inhibitor (pIC50 = 6 in human recombinant ion-leaky assays).
  4. BCRP inhibitor

    Ko 143 is potent and selective inhibitor of breast cancer resistance protein multidrug transporter (BCRP) with an EC90 value of 26 nM.
  5. Gardos channel blocker

    Senicapoc (ICA-17043) is a potent and selective Gardos channel blocker with IC50 value of 11 nM. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
  6. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  7. Vernakalant 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.
  8. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  9. Proton Pump inhibitor

    Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion.
  10. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  11. Voltage-gated sodium channels antagonist

    Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
  12. Amiloride hydrochloride dihydrate is a potent epithelial sodium channel blocker and selective low threshold (T-type) calcium channel protein inhibitor (KD=30μM).
  13. Lacidipine is a calcium channel blocker
  14. Benidipine hydrochloride is a long-acting T-type calcium channel blocker, on blood pressure and renal function in hypertensive patients with diabetes mellitus.
  15. calcium channel blocker

    Nilvadipine is a calcium channel blocker (CCB) used for the treatment of hypertension and chronic major cerebral artery occlusion
  16. Calcium channel blocker

    Clevidipine is a dihydropyridine calcium channel blocker indicated for the reduction of blood pressure when oral therapy is not feasible or not desirable.
  17. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
  18. Ivabradine Hydrochloride, also known as S-16257, is the hydrochloride salt preparation of Ivabradine, a bradycardic agent.
  19. Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
  20. KATP channel antagonist

    Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
  21. Na+/Ca2+ Exchanger Inhibitor

    KB-R7943 mesylate is a cell permeable, potent, selective NCKX inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1.
  22. KCa3.1 channel activator

    NS 309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels).
  23. Cynarin is a phenolic compound found in artichoke. It has antioxidant and choleretic properties. It is a potential immunosuppressive agent.
  24. Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
  25. Resibufogenin is a specific Na+/K+-ATPase inhibitor.
  26. Bufotalin is a less potent Na+/K+-ATPase inhibitor than other bufadienolides. Potent immunosuppressor.
  27. Cinobufagin is a specific Na+/K+-ATPase inhibitor. About as active as ouabain
  28. T-type calcium channel inhibitor

    MK-8998 (compound 33) is a potent and selective inhibitor of the T-type calcium channel.
  29. Nav inhibitor

    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
  30. Ca2+ channel agonist/CDK2 inhibitor

    Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  31. P-gp inhibitor

    Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
  32. Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
  33. Sodium channel blocker

    Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.
  34. 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.
  35. P-gp inhibitor

    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  36. Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2).
  37. Serotonin transporter inhibitor

    Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter.
  38. SGLT2 Inhibitor

    Luseogliflozin is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM).
  39. TRPV1 receptor antagonist

    A-889425 is a selective TRPV1 receptor antagonist. A-889425 blocks TRPV1 channels with an IC50 of 335 nM (rat) and 34 nM (human).
  40. CFTR inhibitor

    IOWH032 is a CFTR inhibitor.
  41. P-gp inhibitor

    ONT-093 is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy.
  42. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
  43. 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.
  44. SGLT2 inhibitor

    Ipragliflozin is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  45. TRPM8 and TRPA1 activator

    Icilin is a cooling agent that activates the novel cold receptors TRPM8 (CMR1) and TRPA1 (ANKTM1/TRPN1), members of the TRP ion channel family. Induces currents in CMR1-expressing HEK 293 cells (EC50 = 0.36 μM)
  46. VMAT2 inhibitor

    GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2), which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles.
  47. ACA is a channel blocker that acts on several transient receptor potential (TRP) channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 uM, respectively).
  48. voltage-gated sodium channel Nav1.7 inhibitor

    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  49. AMPA desensitization inhibitor

    Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 M).
  50. CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.

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