Membrane Transporters-Ion Channels

Items 51-100 of 609

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  1. Myosin activator

    CK-1827452 is a selective cardiac specific myosin activator.
  2. calcium channel blocker

    Azelnidipine is a calcium blocker that attenuates liver fibrosis and may increase antioxidant defence. that attenuates liver fibrosis and may increase antioxidant defence.
  3. Sodium channel Blocker

    A 803467 is a selective blocker of NaV1.8 channels (IC50 values are 8, 2450, 6740, 7340 and 7380 nM for hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels respectively).
  4. potassium-competitive acid Blocker

    TAK-438 is a novel potassium-competitive acid blocker.
  5. 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.
  6. K+/Na+/Ca+ Channel Blocker

    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
  7. 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.
  8. ATPase antagonist

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

    Ko 143 is potent and selective inhibitor of breast cancer resistance protein multidrug transporter (BCRP) with an EC90 value of 26 nM.
  10. 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.
  11. 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.
  12. P-gp inhibitor

    Tariquidar (XR9576) is a P-glycoprotein drug efflux pump inhibitor.
  13. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  14. 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.
  15. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  16. Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion.
  17. NMDA receptor antagonist

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

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

    Nilvadipine is a calcium channel blocker (CCB) used for the treatment of hypertension and chronic major cerebral artery occlusion
  23. 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.
  24. 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.
  25. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
  26. Ivabradine Hydrochloride, also known as S-16257, is the hydrochloride salt preparation of Ivabradine, a bradycardic agent.
  27. 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.
  28. KATP channel antagonist

    Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
  29. 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.
  30. KCa3.1 channel activator

    NS 309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels).
  31. 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.
  32. Cynarin is a phenolic compound found in artichoke. It has antioxidant and choleretic properties. It is a potential immunosuppressive agent.
  33. 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.
  34. Resibufogenin is a specific Na+/K+-ATPase inhibitor.
  35. Bufotalin is a less potent Na+/K+-ATPase inhibitor than other bufadienolides. Potent immunosuppressor.
  36. Cinobufagin is a specific Na+/K+-ATPase inhibitor. About as active as ouabain
  37. T-type calcium channel inhibitor

    MK-8998 (compound 33) is a potent and selective inhibitor of the T-type calcium channel.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. Sodium channel blocker

    Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.
  43. 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.
  44. TRPC6 inhibitor

    TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
  45. P-gp & BCRP inhibitor

    Elacridaris a prototypical BCRP inhibitor which inhibits the Bcrp1-mediated transport.
  46. NHE3 inhibitor

    NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
  47. T-type Ca2+ channel blocker

    ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  48. 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.
  49. Ampalex is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator
  50. 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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