Membrane Transporters-Ion Channels

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Product Citation
  1. 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.
  2. 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.
  3. Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.
  4. Calcium channel blocker

    Berbamine is a calcium channel blocker.
  5. Ca 2+ /Mg 2+ -ATPase inhibitor

    Glucagon (19-29) (human) is a potent Ca 2+ /Mg 2+ -ATPase inhibitor.
  6. Calcium channel blocker

    (S)-Amlodipine is a (S)-Enantiomer of Amlodipine and a dihydropyridine calcium channel blocker with activity resides mainly in the (-)-isomer.
  7. 20-HETE is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells.
  8. serotonin reuptake inhibitor

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

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

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  11. Calcium-Sensing Receptor Antagonist

    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  12. 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.
  13. 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.
  14. Cardiac Na+ channel blocker

    Flecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
  15. Na+,K+-ATPase inhibitor

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

    Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  17. CFTR potentiator

    Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  18. M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel. Antiviral agents.
  19. Calcium channel blocker

    NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
  20. N-type calcium channel blocker

    NP118809 is a potent N-type calcium channel blockers(IC50= 0.11 uM) ; good selectivity over L-type calcium channels.
  21. 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).
  22. 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).
  23. 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.
  24. AMPA antagonist

    Tezampanel is an antagonist at the AMPA and kainate families of ionotropic glutamate receptors, with selectivity for the GluR5 subtype of the kainate receptor.
  25. Ion channel blocker

    Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
  26. P-gp inhibitor

    Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  27. Potassium channel blocker

    Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β.
  28. Slows neuronal Na+ channel inactivation

    beta-Pompilidotoxin is a peptide with the sequence H2N-Arg.
  29. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  30. Na+-glucose transporter inhibitor

    T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
  31. 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.
  32. 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).
  33. TMEM16A Inhibitor

    T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells.
  34. ATPase and GTPase inhibitor

    Etidronate Disodium is a bisphosphonate bone resorption inhibitor.
  35. hERG1 potassium channel activator

    KB130015 is a novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages.
  36. AMPA antagonist

    YM90K hydrochloride is a selective AMPA receptor antagonist that delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration.
  37. Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
  38. TRPA1 activatior/TRPM8 blocker

    Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility.
  39. TRPV1 modulator

    MRS1477 is a TRPV1 positive allosteric modulator.
  40. KV7.2/7.3 activator

    ICA-110381 is a KV7.2/7.3 activator with EC50 of 0.38 uM.
  41. AMPA/kainate receptor antagonist

    Talampanel is a non-competitive antagonist of AMPA-receptor.
  42. TRPC4/C5 inhibitor

    ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
  43. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
  44. TRPV1 antagonist

    Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
  45. 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.
  46. MCT Inhibitor?€?

    7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
  47. TRPM8 antagonist

    RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
  48. F508del-CFTR trafficking corrector

    KM 11060 corrects F508del-CFTR trafficking, increasing the amount of functional CFTR at the plasma membrane (~75%) and Inhibits PDE5 activity
  49. TRPV4 Activator

    GSK1016790A is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
  50. TRPV1 receptor antagonist

    SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist.

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