Membrane Transporters-Ion Channels

Items 451-500 of 2532

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  1. TRP Channel blocker

    SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
  2. elastogenesis inhibitor

    L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
  3. Na+/Ca2+ exchange Inhibitor

    CGP 37157 is a benzothiazepine that acts as a selective inhibitor of the mitochondrial sodium-calcium exchanger (IC50 = 0.36 μM in isolated mitochondria).
  4. CRAC channel inhibitor

    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  5. plasmodium ATP4 inhibitor

    (+)-SJ733 is an inhibitor of plasmodium ATP4, leading to rapid clearance in vivo by inducing physical changes in infected, treated red cells.
  6. Coelenterazine h is a derivative of Coelenterazine. Coelenterazine h is more sensitive to Ca2+ than is the native complex, thus providing a valuable tool for measuring small changes in Ca2+ concentrations.
  7. SERCA2 allosteric activator

    CDN1163 is a SERCA2 allosteric activator. It increases Ca2+-ATPase activity and Ca2+ uptake by ER microsomes from obese mice. Rescues HEK cells from ER stress-induced cell death.
  8. TREK-1/2 Activator

    ML335 is a potent and selective TREK-1/2 Activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
  9. chloride channel blocker

    NPPB is a chloride channel blocker (IC50 = 80 nM) that has also been identified as a GPR35 agonist.
  10. TRPV1 antagonist

    A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
  11. P-glycoprotein inhibitor

    Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
  12. BCRP inhibitor

    YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.
  13. SGLT2 inhibitor

    Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  14. NAADP antagonist

    Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca2+ signaling, with an IC50 of 65 nM.
  15. Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
  16. triple reuptake inhibitor

    Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  17. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
  18. Nav1.7 sodium channel inhibitor

    Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
  19. AMPA/kainate antagonist

    Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
  20. HCN channels inhibitor

    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 ?M.
  21. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  22. F1F0-ATPase modulator

    Bz-423 is an F1F0-ATPase modulator. It acts by selectively killing autoimmune lymphocytes.
  23. iron mobilizer

    Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  24. KCa1.1 channels activator

    NS 11021 is a potent and specific Ca2-activated big-conductance K?? Channels (KCa1.1 channels) activator.
  25. AMPA receptors potentiator

    Mibampator (LY451395) is a potent and highly selective potentiator of the AMPA receptors.
  26. T-type Ca2+ channel antagonist

    TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
  27. TASK1(KCNK3) inhibitor

    ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).
  28. AMPAR antagonist

    Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
  29. KCNQ1 potassium channel activator

    ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
  30. CRM1 inhibitor

    Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.
  31. Ca2+-dependent blocker

    TV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
  32. CARC blocker

    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  33. Na+/H+ exchange inhibitor

    Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na+/H+ exchange inhibitor.
  34. AMPA receptors allosteric modulator

    PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
  35. non-narcotic antitussive

    Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
  36. AMPA receptors positive allosteric modulator

    CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ?? 4.2 nM/63.4 ?? 5.6 nM for GluA2i/GluA2o receptor.
  37. AMPA (CP-AMPA) receptors antagonist

    Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
  38. positive AMPAR modulator

    CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.
  39. TRPC3 inhibitor

    Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
  40. non-competitive AMPAR antagonist

    CFM-2 is a selective non-competitive AMPAR antagonist.
  41. L-type calcium antagonist

    Barnidipine (Mepirodipine) 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.
  42. AMPA/kainate receptors agonist

    (S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
  43. N- and P/Q-type Ca2+ channels agonist

    GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
  44. Na+ channel blocker

    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
  45. sphingomyelin synthase inhibitor

    Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors.
  46. SGLT1 inhibitor

    Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1.
  47. TRPV1 antagonist

    PF-04745637 is a TRPV1 antagonist.
  48. SGLT1 inhibitor

    KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively.
  49. CRAC inhibitor

    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
  50. HCN4 CLP ligand

    BPU-11 is a HCN4 CLP ligand. It acts by modulating channel function and completely abolishing the cAMP-induced shift in V1/2.

Items 451-500 of 2532

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