Membrane Transporters-Ion Channels

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Product Name
Application
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Product Citation
  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. TRPC1/4/5 channels inhibitor

    Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
  4. 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. MCT inhibitor

    CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.
  6. P-gp inhibitor

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

    Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter.
  8. 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).
  9. CFTR inhibitor

    IOWH032 is a CFTR inhibitor.
  10. 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.
  11. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
  12. 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.
  13. 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.
  14. 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.
  15. myosin II inhibitor

    Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
  16. 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).
  17. CFTR inhibitor

    CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).
  18. 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).
  19. VDAC inhibitor

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
  20. hASBT inhibitor

    GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor.
  21. 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.
  22. 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.
  23. sodium channel protein inhibitor

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

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

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

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  27. 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.
  28. NHE3 inhibitor

    Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.
  29. Na(+)/H(+) exchange inhibitor

    ENIPORIDE is a potent Na+/H+ exchange inhibitor.
  30. MCT1 inhibitor

    AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.
  31. Sodium channel blocker/DNMT inhibitor

    Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor.
  32. sodium-potassium pump inhibitor

    Digoxin is a sodium-potassium pump inhibitor.
  33. proton pump inhibitor

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

    BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
  35. 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.
  36. 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.
  37. Ca 2+ /Mg 2+ -ATPase inhibitor

    Glucagon (19-29) (human) is a potent Ca 2+ /Mg 2+ -ATPase inhibitor.
  38. serotonin reuptake inhibitor

    Azaphen is a potent inhibitor of the reuptake of serotonin.
  39. Glycine reuptake inhibitor

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  40. Glycine reuptake inhibitor

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  41. P-gp inhibitor

    Elacridar hydrochloride is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.
  42. Proton pump inhibitor

    Esomeprazole Magnesium trihydrate is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  43. Na+,K+-ATPase inhibitor

    Istaroxime (PST2744) is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM.
  44. NBC inhibitor

    S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM).
  45. NCX inhibitor

    SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger with IC50 of 5-33 nM (inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia).
  46. Sodium Channel inhibitor

    Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
  47. P-gp inhibitor

    Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  48. Na+-glucose transporter inhibitor

    T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
  49. elastogenesis inhibitor

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

    CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells).

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