Membrane Transporters-Ion Channels

Items 551-600 of 2532

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  1. nuclear export receptor CRM1 inhibitor

    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
  2. ROMK inhibitor

    MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
  3. Sunifiram (DM-235) is a piperazine derived ampakine-like drug which has nootropic effects in animal studies with significantly higher potency than piracetam.
  4. dual NE/DA transporter inhibitor

    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  5. URAT1 inhibitor

    Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor with an IC50 of 25 nM.
  6. Nav1.7 inhibitor

    Nav1.7 inhibitor is a potent Nav1.7 inhibitor.
  7. AMPA receptor positive allosteric modulator

    PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.
  8. calcium channel inhibitor

    Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM).
  9. L-type Ca2+ channel agonist

    (S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM).
  10. calcium-sensing receptor (CaR) antagonist

    SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.
  11. AMPA antagonist

    Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
  12. glutamate receptor subtype antagonist

    Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
  13. AMPA/kainate antagonist

    Fanapanel (ZK200775) 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.
  14. TRPV1 receptor antagonist

    Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
  15. P-glycoprotein inhibitor

    Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
  16. phenylalkylamine calcium antagonist

    Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist.
  17. Serotonin reuptake inhibitor (SSRI)

    Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.
  18. mitoKATP channels

    BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.
  19. KATP activator

    Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator.
  20. Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.

  21. Sodium Channel Nav1.7 inhibitor

    Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
  22. H+/K+-ATPase inhibitor

    Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1??0.4 μM.
  23. NHE1 inhibitor

    BI-9627 is a sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor with an EC50 of 31 nM.
  24. Piezo1 agonist

    Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.
  25. AMPAR agonist

    (S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR agonist.
  26. hERG potassium channel inhibitor

    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  27. T-type Ca2+ channel antagonist

    TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
  28. potassium channel inhibitor

    VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  29. HCN channels inhibitor

    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 ?M.
  30. Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
  31. Calcium channel blocker

    Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
  32. dual T-type and L-type calcium channel blocker

    Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB).
  33. CP-AMPA receptors antagonist

    Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
  34. TRPP3 channel inhibitor

    EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
  35. P-glycoprotein/MRP-1 modulator

    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  36. calcium antagonist

    Palonidipine is a calcium antagonist which is potential for the therapy of angina-pectoris and hypertension.
  37. TRPC4/TRPC5 antagonist

    HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.
  38. CFTR potentiator

    GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
  39. benzazepine calcium channel blocker

    SQ-31765 is a benzazepine calcium channel blocker.
  40. TRPC6 inhibitor

    DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
  41. TRPV1 antagonist

    AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
  42. TREK-1 activator

    ML402 is a selective TREK-1 activator.
  43. potassium channel (non-GIRK1/X) activator

    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  44. NecroX-5 is a derivative of the NecroX, reduces intracellular calcium concentration, and possesses anti-inflammatory and anti-cancer activity.
  45. CRM1 inhibitor

    CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities.
  46. NaV1.7 inhibitor

    GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
  47. mitochondrial protonophore uncoupler

    BAM 15 is a novel mitochondrial protonophore uncoupler.
  48. TARP γ-8 negative modulator

    AMPA Receptor Modulator-1 is a potent, oral active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
  49. TRPA1 antagonist

    TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC50 of 8 nM.
  50. Transmembrane glutamine flux antagonist

    V-9302 is a competitive antagonist of transmembrane glutamine flux.

Items 551-600 of 2532

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