Membrane Transporters-Ion Channels

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  1. 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).
  2. non-competitive AMPAR antagonist

    CFM-2 is a selective non-competitive AMPAR antagonist.
  3. 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.
  4. AMPA/kainate receptors agonist

    (S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
  5. 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.
  6. Na+ channel blocker

    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
  7. 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.
  8. 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.
  9. TRPV1 antagonist

    PF-04745637 is a TRPV1 antagonist.
  10. 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.
  11. CRAC inhibitor

    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
  12. 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.
  13. inhibitor of Kv2.1 and Kv2.2

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

    Levobupivacaine hydrochloride is a sodium channel blocker.
  15. VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum (SR) Ca(2+) release but does not block the β-receptor.
  16. 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.
  17. antagonist of Vanilloid receptor type 1

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

    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties.
  19. 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.
  20. 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.
  21. VDAC1/Apoptosis inhibitor

    NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. MCU modulator

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

    ATPO is a potent and Selective Ampa Receptor Antagonist.
  28. Calcium channel blocker

    Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

  29. Calcium channel antagonist

    Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.

  30. potassium currents blocker

    Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. 

  31. AQP4 inhibitor

    AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke.
  32. TRPM8 antagonist

    M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively).
  33. TRPV1 antagonist and TNF-alpha production inhibitor

    LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor.
  34. ROMK inhibitor

    VU590 is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 is not a good probe of ROMK function in the kidney.
  35. blocker of fast Na+-dependent action potentials and voltage-dependent

    Lidocaine N-ethyl bromide is a non-membrane-permeable blocker of fast Na+-dependent action potentials and voltage-dependent, non-inactivating Na+ conductance.
  36. KCNQ2/3 potassium channels activator

    QO-40 is an activator of KCNQ2/3 potassium channels.
  37. Ca2+-activated K+ channel activator

    NS19504 is a Ca2+-activated K+ channel (BK channel, KCa1.1 channel) activator (EC50=11.0 μM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.

  38. potassium current activator

    NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
  39. vasodilator drug

    Pentamethonium bromide is a vasodilator drug.
  40. TRPM8 channel blocker

    TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells
  41. Beta1-Adrenergic receptor antagonist

    Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

  42. Oct3/4 inducer

    Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells.
  43. CRM1-selective inhibitor

    Selinexor trans-isomer is a trans-isomer of Selinexor or KPT-330, which is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.
  44. VMAT-2 inhibitor

    Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2).
  45. Potassium Channel inhibitor

    Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion.
  46. V-ATPase inhibitor

    KM 91104 is a cell-permeable inhibitor of V-ATPase that specifically targets the interaction between V-ATPase subunit a3 and subunit B2.
  47. VDAC Inhibitor

    DIDS sodium salt is a potent inhibitor of voltage-dependent anion channels (VDAC1) and also targets the ABCA1 transporter. This compound effectively disrupts RAD51-mediated homologous pairing and strand exchange reactions, making it valuable for studying DNA repair mechanisms. Additionally, DIDS is known to inhibit anion exchange and interfere with caspase-3 and -9 activation, facilitating its application in cancer research and apoptosis studies.
  48. CDK Inhibitor

    Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders.
  49. Serotonergic Receptor Antagonist

    Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology.
  50. K+ Channels Activator

    1-EBIO is an activator of Ca2+-sensitive K+ channels, playing a crucial role in the modulation of membrane potential and cellular excitability. This compound is utilized in research to investigate the physiological functions and pathophysiological roles of K+ channels, contributing to a deeper understanding of cellular signaling processes and potential therapeutic targets in various diseases.

Items 101-150 of 2532

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