Membrane Transporters-Ion Channels

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  1. Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. F1F0-ATPase modulator

    Bz-423 is an F1F0-ATPase modulator. It acts by selectively killing autoimmune lymphocytes.
  9. 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.
  10. KCa1.1 channels activator

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

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

    TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
  13. 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).
  14. AMPAR antagonist

    Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
  15. 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.
  16. CRM1 inhibitor

    Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.
  17. 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.
  18. 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.
  19. Na+/H+ exchange inhibitor

    Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na+/H+ exchange inhibitor.
  20. 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.
  21. non-narcotic antitussive

    Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
  22. 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.
  23. 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.
  24. positive AMPAR modulator

    CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.
  25. 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).
  26. non-competitive AMPAR antagonist

    CFM-2 is a selective non-competitive AMPAR antagonist.
  27. 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.
  28. AMPA/kainate receptors agonist

    (S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
  29. 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.
  30. Na+ channel blocker

    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
  31. 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.
  32. 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.
  33. TRPV1 antagonist

    PF-04745637 is a TRPV1 antagonist.
  34. 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.
  35. CRAC inhibitor

    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
  36. 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.
  37. inhibitor of Kv2.1 and Kv2.2

    RY785 (Kv2-IN-A1) is an inhibitor of Kv2.1 and Kv2.2.
  38. sodium channel blocker

    Levobupivacaine hydrochloride is a sodium channel blocker.
  39. VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum (SR) Ca(2+) release but does not block the β-receptor.
  40. OPRM1/OPRD1 agonist

    ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively.
  41. antagonist of Vanilloid receptor type 1

    A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1).
  42. TRPC5 inhibitor

    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties.
  43. anticancer agent

    Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition.
  44. anticancer agent

    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  45. VDAC1/Apoptosis inhibitor

    NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.
  46. ATPase activator

    Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
  47. glutamine transporter ASCT2 inhibitor

    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor.
  48. Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators.
  49. Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.
  50. MCU modulator

    MCU-i4 is a novel negative modulator of the MCU, binding MICU1 and impairing muscle cell growth.

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