Membrane Transporters-Ion Channels

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Citations
  1. VRAC inhibitor

    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC), voltage-dependently activates potassium channels TREK1 and TRAAK, inhibits TRESK, TASK1 and TASK3 (IC50s, 0.14, 0.95, 50.72 μM, respectively).
  2. L-type calcium antagonist

    Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
  3. NaV1.8 blocker

    PF 04531083 is a selective NaV1.8 blocker, and used for the research of neuropathic/inflammatory pain.
  4. CRAC channel inhibitor

    Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.
  5. Calcium Channel antagonist

    Fantofarone is a highly potent Calcium Channel antagonist.
  6. VSCC blocker

    PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
  7. NAADP antagonist and TPC blocker

    trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
  8. TRPM8 antagonist

    TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
  9. Kv3 voltage-gated potassium channel modulator

    Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 can be used to treat inflammatory pain.
  10. Ca2+ channel blocker

    MRS1845 is a Ca2+ channel blocker with relative specificity for store-operated calcium entry (SOCE) channels.
  11. Dotinurad is a potent uricosuric agent, with an IC50 of 3.6 ?M for uric acid.
  12. T-type calcium channel inhibitor

    ML218 is a selective T-type calcium channel inhibitor with IC50s of 270 and 310 nM for Cav3.3 and Cav3.2 in electrophysiology assay, respectively.
  13. ligand for the α2δ subunit of voltage-gated calcium channels

    Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
  14. SGLT2 inhibitor

    Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.
  15. ecto-ATPase inhibitor

    ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively.
  16. H+/K+-ATPase inhibitor

    SCH28080 inhibits gastric H+/K+-ATPase by K+-competitive binding, with an IC50 value of 20 nM in rabbit microsomal membranes. Antisecretory and cytoprotective activities.
  17. TRPM8 antagonist

    AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
  18. CRAC inhibitor

    CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
  19. TRPA1 agonist

    JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.
  20. CatSper channels blocker

    HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 ?M).
  21. calcium channel blocker

    ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
  22. 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.
  23. Calcium channel blocker

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

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

    (S)-Amlodipine is a (S)-Enantiomer of Amlodipine and a dihydropyridine calcium channel blocker with activity resides mainly in the (-)-isomer.
  26. 20-HETE is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells.
  27. serotonin reuptake inhibitor

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

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

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

    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  31. 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.
  32. 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.
  33. 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.
  34. Na+,K+-ATPase inhibitor

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

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

    Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
  37. M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel. Antiviral agents.
  38. 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.
  39. 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.
  40. 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).
  41. 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.
  42. 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.
  43. P-gp inhibitor

    Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  44. 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.
  45. Slows neuronal Na+ channel inactivation

    beta-Pompilidotoxin is a peptide with the sequence H2N-Arg.
  46. 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).
  47. Na+-glucose transporter inhibitor

    T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
  48. 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.
  49. 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).
  50. TMEM16A Inhibitor

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

Items 301-350 of 2532

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