Membrane Transporters-Ion Channels

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  1. 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).
  2. 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).
  3. 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.
  4. 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.
  5. Protein translocation Inhibitor

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

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

    Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor.
  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. 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.
  11. T-type calcium channel inhibitor

    MK-8998 (compound 33) is a potent and selective inhibitor of the T-type calcium channel.
  12. 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.
  13. 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.
  14. 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.
  15. P-gp inhibitor

    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  16. Serotonin transporter inhibitor

    Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter.
  17. 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).
  18. CFTR inhibitor

    IOWH032 is a CFTR inhibitor.
  19. 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.
  20. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
  21. 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.
  22. 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.
  23. 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.
  24. 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).
  25. NaV1.3 and NaV1.1 channels inhibitor

    ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively).
  26. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  27. Na+/K+ ATPase inhibitor

    Melittin is a Na+/K+ ATPase inhibitor. It inhibits Gs and stimulates Gi activity. It inhibits protein kinase C and cAMP-dependent protein kinases.
  28. Ca2+ release inhibitor

    Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor.
  29. sodium channel protein inhibitor

    Oxcarbazepine is a sodium channel protein inhibitor.
  30. P-glycoprotein inhibitor

    XR9576 is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer
  31. SGLT2 inhibitor

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

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  33. 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.
  34. 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).
  35. Na(+)/H(+) exchange inhibitor

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

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

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

    BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
  39. 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.
  40. 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.
  41. Pgp1 inhibitor

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

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

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

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  45. 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.
  46. proton pump inhibitor

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

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

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  49. 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.
  50. 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.

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