Membrane Transporters-Ion Channels

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  1. SGLT2 inhibitor

    Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney.
  2. ATP synthase inhibitor

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  3. SERCA inhibitor

    Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels.
  4. TrxR1/CRM1 inhibitor

    Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1).
  5. Na(+)/H(+) exchange inhibitor

    ENIPORIDE is a potent Na+/H+ exchange inhibitor.
  6. Sodium channel blocker/DNMT inhibitor

    Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor.
  7. proton pump inhibitor

    Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 uM.
  8. F1 Fo-ATPase inhibitor

    BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
  9. MCT1 inhibitor

    AR-C117977 is a potent MCT1 inhibitor, which can reduce vimmune responses both in vitro and in vivo, maintains long-term graft survival, and induces operational tolerance.
  10. late INa Inhibitor

    GS967 is a novel, potent, and selective inhibitor of cardiac late sodium current(late INa); inhibits ATX-II-induced late I(Na) in ventricular myocytes and isolated hearts with IC(50) values of 0.13 and 0.21 uM, respectively.
  11. Pgp1 inhibitor

    NSC 23925 is a plasma membrane glycoprotein 1 (Pgp1) inhibitor to reverse multidrug resistance (MDR1).
  12. NHE-1 inhibitor

    Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na+/H+ exchanger (NHE-1).
  13. BCRP/ABCG2 inhibitor

    YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2).
  14. exportin-1 inhibitor

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  15. 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.
  16. proton pump inhibitor

    Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
  17. H(+)-K(+)-exchanging ATPase inhibitor

    Rabeprazole is an inhibitor of H(+)-K(+)-exchanging atpase in gastric parietal cells.
  18. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  19. Calcium channel proteins inhibitor

    Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
  20. SChE inhibitor

    Dibucaine (USAN) is an amide local anesthetic. Dibucaine reversibly binds to and inactivates sodium channels in the neuronal cell membrane. Inhibition of sodium channels prevents the depolarization of nerve cell membranes and inhibits subsequent propagation of impulses along the course of the nerve, thereby limiting the excitation of nerve endings. This results in loss of sensation.
  21. SGLT2 inhibitor

    Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine.
  22. SGLT2 inhibitor

    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2.
  23. SGLT inhibitor

    Ertugliflozin pidolate belongs to the class of potent and selective inhibitors of the sodium-dependent glucose cotransporters (SGLT), more specifically the type 2 which is responsible for about 90% of the glucose reabsorption from glomerulus.
  24. IP3R inhibitor

    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
  25. proton pump inhibitor

    Lansoprazole sodium(AG-1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  26. VDAC inhibitor

    WEHI-9625 is a tricyclic sulfone small molecule inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK, but is completely inactive against both human BAK and the closely related apoptosis effector BAX.
  27. P-gp/BCRP dual inhibitor

    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
  28. 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.
  29. 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.
  30. 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.
  31. SUR/URAT1 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.
  32. sodium channel inhibitor

    Levobupivacaine is a local anaesthetic drug belonging to the amino amide group.
  33. p97 ATPase inhibitor

    ML241 is a potent and selective inhibitors of p97 ATPase. ML241 inhibit p97 ATPase with IC(50) values of 100 nM.
  34. HIV integrase inhibitor

    GSK744 is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.
  35. P-gp inhibitor

    MC-70 is a potent P-gp inhibitor (EC50 = 0.69 uM).
  36. voltage-gated sodium channel inhibitor

    Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties.
  37. proton pump inhibitor

    Rabeprazole sodium is an antiulcer drug in the class of proton pump inhibitors.
  38. K+ Channel inhibitor

    K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur).
  39. URAT1 inhibitor

    UR 1102, inhibitor of the renal urate transporter URAT1 with high selectivity to URAT1 over OAT1 and OAT3 in vitro (Ki values 0.057 uM, 7.2 uM, and 2.4 uM, respectively), capable of increasing the fractional excretion of urinary uric acid, and reducing plasma uric acid more effectively than Benzbromarone.
  40. BCRP inhibitor

    KS-176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 uM in Pheo A and Hoechst 33342 assays respectively).
  41. VMAT2 inhibitor

    Valbenazine is a potent and selective VMAT2 inhibitor.
  42. Wnt/beta-catenin inhibitor

    Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ?? 1.29 uM; also is an inhibitor of Wnt/beta-catenin signaling.
  43. SINE/CRM1 inhibitor

    KPT276, analog of KPT-185, is a selective inhibitor of nuclear export (SINE) and CRM1.
  44. CRAC channel inhibitor

    YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.
  45. Proton pump inhibitor

    Lauric acid is a proton pump inhibitor potentially for the treatment of helicobacter pylori infections.
  46. Nav1.7 Inhibitor

    PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV.
  47. proton pump inhibitor

    (R)-Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid.
  48. Kir2 family channels inhibitor

    ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
  49. GlyT inhibitor/NMDA receptor

    Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
  50. elastogenesis inhibitor

    L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.

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