Membrane Transporters-Ion Channels

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  1. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
  2. P-gp modulator

    Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  3. 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.
  4. TRPM8 and TRPA1 activator

    Icilin is a cooling agent that activates the novel cold receptors TRPM8 (CMR1) and TRPA1 (ANKTM1/TRPN1), members of the TRP ion channel family. Induces currents in CMR1-expressing HEK 293 cells (EC50 = 0.36 μM)
  5. 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.
  6. ACA is a channel blocker that acts on several transient receptor potential (TRP) channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 uM, respectively).
  7. 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.
  8. 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).
  9. CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
  10. Sodium channel Blocker

    QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltage-activated Na+ channel blocker
  11. 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).
  12. AMPA receptor modulator

    Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia and Alzheimer's Disease. It was found to improve short-term memory, but impaired episodic memory.
  13. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  14. NMDA receptor antagonist

    DNQX is a non-N-methyl-D-aspartate (non-NMDA) receptor complex antagonist.
  15. Sodium channel blocker

    Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.
  16. 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.
  17. 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.
  18. sodium channel protein inhibitor

    Oxcarbazepine is a sodium channel protein inhibitor.
  19. KCa2.1 channels activator

    GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2).
  20. P-glycoprotein inhibitor

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

    Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney.
  22. Selective calcium chelator

    BAPTA tetrapotassium is a selective calcium chelator with greater affinity for Ca2+ than Mg2+.
  23. TrpA1 channel agonist

    PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models.
  24. ATP synthase inhibitor

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  25. 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.
  26. AMPA Receptor Blocker

    IEM 1754 Dihydrobromide is a voltage-dependent open-channel blocker of AMPA receptors.
  27. H3R antagonist/TRPV1 antagonist

    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
  28. 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).
  29. TRPA1 channel blocker

    TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.
  30. Na(+)/H(+) exchange inhibitor

    ENIPORIDE is a potent Na+/H+ exchange inhibitor.
  31. TRPV4 blocker

    GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.
  32. Sodium channel blocker/DNMT inhibitor

    Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor.
  33. Chloroprocaine HCl is a local anesthetic during surgical procedures.
  34. proton pump inhibitor

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

    BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
  36. 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.
  37. 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.
  38. TRPA1 Antagonist

    AM-0902 is a potent and selective Transient Receptor Potential A1 (TRPA1) Antagonist.
  39. AMPA antagonist

    GYKI53655 Hydrochloride is a non-competitive AMPA and kainate receptor antagonist. CAS: 143692-18-6 (Free Base); 143692-48-2 (HCl).
  40. TRPM8 Agonist

    WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 = 193 nM).
  41. TRPM8 agonist

    WS 3 is TRPM8 receptors agonist (EC50 = 3.7 μM) and cooling agent.
  42. Pgp1 inhibitor

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

    Rimeporide (EMD-87580) is a potent and selective inhibitor of the Na+/H+ exchanger (NHE-1).
  44. potassium channel activator

    SKA-31 is an activator of KCa2 and KCa3.1 calcium-activated potassium channels.
  45. BCRP/ABCG2 inhibitor

    YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2).
  46. TRPM8 Antagonist

    AMG-333 is a potent and selective TRPM8 Antagonist.
  47. exportin-1 inhibitor

    Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.
  48. 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.
  49. proton pump inhibitor

    Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.
  50. Nonivamide is a capsaicin analogue that exhibits anti-inflammatory properties in peripheral blood mononuclear cells and U-937 macrophages. Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.

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