Membrane Transporters-Ion Channels

Items 251-300 of 2532

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  1. Oct3/4 Inducer

    O4I1 increases Oct3/4 mRNA levels in HEK293 cells by 2.5- and 4-fold at 10 uM and 20 uM, respectively.
  2. CFTR chloride channel inhibitor

    PPQ-102 is a compound that targets intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR- mediated chloride current in a voltage-dependent and reversible manner.
  3. IBAT inhibitor

    S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.
  4. Sodium channel blocker

    Raxatrigine (GSK1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A.
  5. ABCB1 (P-gp/MDR1) inhibitor

    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity.
  6. MCT Inhibitor

    UK 5099 is a potent inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC); inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.
  7. Istaroxime hydrochloride is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).

  8. EAAT1 inhibitor

    UCPH 101 is a selective non-substrate inhibitor of EAAT1 (IC50 values are 660, >300000 and >300000 nM for EAAT1, EAAT2 and EAAT3 respectively).
  9. intracellular Ca2+ handling modulator

    Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
  10. dihydropyridine calcium entry blocker

    Lemildipine is a new dihydropyridine calcium entry blocker.
  11. Calcium channel blocker

    Amlodipine aspartic acid impurity is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties.
  12. TRPA1 inhibitor

    HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 = 6.2 and 5.3 uM, respectively).
  13. Na+/K+ ATPase modulator

    Rostafuroxin (PST-2238) is an ouabain-inhibitor counteracting specific forms of hypertension.
  14. Monocrotaline is a natural 11-membered macrocyclic pyrrolizidine alkaloid used in an animal model of pulmonary hypertension.
  15. AMPA antagonist

    CP 465022 is a selective, non-competitive AMPA antagonist with IC50 of 25 nM in rat cortical neurons that displays potent anticonvulsant activity.
  16. COX inhibitor

    Flufenamic acid is a nonsteroidal anti-inflammatory drug (NSAID). Inhibits calcium-activated chloride channels (CaCCs). Also increases currents through TRPC6 channels and inhibits currents through TRPC3 and TRPC7 channels.
  17. CaCC blocker

    Talniflumate is a calcium-activated chloride channel (CaCC) (hCLCA1/mCLCA3) blocker; reduces mucin synthesis and release in cell culture and animal models.
  18. BCH

    LAT1 inhibitor

    BCH is an inhibitor of L-type amino acid transporter LAT1. Suppresses growth and induces apoptosis via activation of caspases in KB, Saos2 and C6 cancer cell lines.
  19. TRPV1 antagonist

    SB-705498 is a potent, selective and orally bioavailable TRPV1 antagonist.
  20. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
  21. 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.
  22. 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).
  23. potassium-competitive acid Blocker

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

    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
  25. 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.
  26. ATPase antagonist

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

    Ko 143 is potent and selective inhibitor of breast cancer resistance protein multidrug transporter (BCRP) with an EC90 value of 26 nM.
  28. 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.
  29. PDE1 inhibitor

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  30. 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.
  31. serotonin transporter (SER) inhibitor

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

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

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

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

    Nilvadipine is a calcium channel blocker (CCB) used for the treatment of hypertension and chronic major cerebral artery occlusion
  39. 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.
  40. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
  41. Ivabradine Hydrochloride, also known as S-16257, is the hydrochloride salt preparation of Ivabradine, a bradycardic agent.
  42. 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.
  43. KATP channel antagonist

    Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
  44. 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.
  45. KCa3.1 channel activator

    NS 309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels).
  46. Cynarin is a phenolic compound found in artichoke. It has antioxidant and choleretic properties. It is a potential immunosuppressive agent.
  47. 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.
  48. Resibufogenin is a specific Na+/K+-ATPase inhibitor.
  49. Bufotalin is a less potent Na+/K+-ATPase inhibitor than other bufadienolides. Potent immunosuppressor.
  50. Cinobufagin is a specific Na+/K+-ATPase inhibitor. About as active as ouabain

Items 251-300 of 2532

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