Membrane Transporters-Ion Channels

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  1. AMPA Receptor Inhibitor

    Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam.
  2. SGLT2 inhibitor

    EGT1442 is a potent and selective SGLT2 inhibitor.
  3. 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.
  4. Proton pump inhibitor

    Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  5. Kir6.2/SUR inhibitor

    Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
  6. proton pump inhibitor

    Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  7. Calcium Channel inhibitor

    Nimodipine is a L-type Ca2+ channel blocker.
  8. ATPase inhibitor

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

    Omeprazole is a cell-permeable, selective proton pump inhibitor.
  10. CFTR Inhibitor

    Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy.
  11. 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.
  12. CFTR inhibitor

    PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.
  13. Potassium Channel inhibitor

    Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell.
  14. protein tyrosine phosphatases inhibitor

    Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
  15. Calcium Channel inhibitor

    Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis.
  16. MDR1/P-gp Inhibitor

    PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
  17. SGLT2 Inhibitor

    Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).
  18. SGLT2 inhibitor

    PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2.
  19. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
  20. 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.
  21. BCRP inhibitor

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

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

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

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  25. 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.
  26. 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.
  27. T-type calcium channel inhibitor

    MK-8998 (compound 33) is a potent and selective inhibitor of the T-type calcium channel.
  28. 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.
  29. 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.
  30. 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.
  31. TRPC6 inhibitor

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

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

    NHE3-IN-1 is a sodium/proton exchanger type 3 (NHE-3) inhibitor extracted from patent WO 2011019784 A1.
  34. 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.
  35. Nav1.7 inhibitor

    AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.
  36. CRM1 inhibitor

    KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.
  37. SGLT Inhibitor?€?

    LX4211 is a Dual SGLT1/SGLT2 Inhibitor
  38. SGLT2 inhibitor

    Tofogliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.
  39. a-K-ATPase inhibitor

    Ouabain is a selective Na+, K+-ATPase inhibitor.
  40. SGLT1/SGLT2 inhibitor

    Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
  41. Na+/H+-exchange inhibitor

    FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
  42. Na+/H+ exchange inhibitor

    Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor.
  43. CFTR inhibitor

    CFTRinh-172 is a voltage-independent, selective CFTR inhibitor
  44. 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.
  45. CRM1 Inhibitor

    KPT185 is a selective CRM1 inhibitor. KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts.
  46. SUR inhibitor

    Lesinurad is a selective uric acid re-absorption inhibitor (SURI) and is also a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body.
  47. 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.
  48. IBAT inhibitor

    S-8921 is an ileal Na+/bile acid cotransporter (IBAT) inhibitor.
  49. 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.
  50. 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.

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