Membrane Transporters-Ion Channels

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  1. KCa1.1 channels activator

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

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

    TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
  4. 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).
  5. AMPAR antagonist

    Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
  6. 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.
  7. CRM1 inhibitor

    Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.
  8. 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.
  9. 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.
  10. Na+/H+ exchange inhibitor

    Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na+/H+ exchange inhibitor.
  11. 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.
  12. non-narcotic antitussive

    Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
  13. 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.
  14. 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.
  15. positive AMPAR modulator

    CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.
  16. 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).
  17. non-competitive AMPAR antagonist

    CFM-2 is a selective non-competitive AMPAR antagonist.
  18. 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.
  19. AMPA/kainate receptors agonist

    (S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
  20. 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.
  21. Na+ channel blocker

    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
  22. 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.
  23. 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.
  24. TRPV1 antagonist

    PF-04745637 is a TRPV1 antagonist.
  25. 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.
  26. CRAC inhibitor

    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
  27. 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.
  28. inhibitor of Kv2.1 and Kv2.2

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

    Levobupivacaine hydrochloride is a sodium channel blocker.
  30. VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum (SR) Ca(2+) release but does not block the β-receptor.
  31. 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.
  32. antagonist of Vanilloid receptor type 1

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

    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties.
  34. 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.
  35. 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.
  36. VDAC1/Apoptosis inhibitor

    NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. MCU modulator

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

    ATPO is a potent and Selective Ampa Receptor Antagonist.
  43. gastric H+/K+ ATPase inhibitor

    Soraprazan is a reversible, and fast-acting inhibitor of gastric H+/K+ ATPase.
  44. Proton Pump inhibitor

    Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition.
  45. KCNQ2/Q3 potassium channel activator

    ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
  46. BCRP inhibitor

    (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
  47. TRPV4 antagonist

    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
  48. Nav1.8 channel blocker

    PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
  49. SGLT1/SGLT2 inhibitor

    LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract.
  50. TRPV4 agonist

    RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.

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