Membrane Transporters-Ion Channels

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  1. HCN channel blocker

    ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
  2. proton pump antagonist

    Pumaprazole is a reversible proton pump antagonist.
  3. SMN2 splicing modulator

    Branaplam (LMI070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.
  4. calcium channel antagonist

    SM-6586 is a calcium channel antagonist and inhibitor of Na+/H+ and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
  5. dihydropyridine Ca2+ antagonist

    CV-159 is a unique dihydropyridine Ca2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
  6. CFTR inhibitor

    (R)-BPO-27 is a potent CFTR inhibitor with an IC50 of 4 nM.
  7. TRPC3 inhibitor

    Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.
  8. TRPV4 ion channel blocker

    GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.
  9. Na+-dependent glutamate transporter inhibitor

    MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
  10. TRPC6 inhibitor

    SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
  11. TRPML3 ion channel activator

    SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8??0.13 μM.
  12. AMPA receptor antagonist

    SYM 2206 is a novel, potent, non-competitive AMPA receptor antagonist.
  13. BTS

    Myosin S1 ATPase Inhibitor

    BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility.
  14. KCC2 inhibitor

    VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).
  15. gastric H+/K+-ATPase inhibitor

    Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro.
  16. Calcium Channel Inhibitor

    Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin.
  17. TRPM8 agonist

    D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
  18. non-voltage dependent calcium channel blocker

    Carboxyamidotriazole (L 651582) is a blocker of non-voltage dependent calcium channel.
  19. Potassium Channel inhibitor

    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  20. IKs blocker

    JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
  21. HIF-1α inhibitor

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
  22. HERG activator

    RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
  23. VMAT2 inhibtior

    NBI-98782(alpha-dihydrotetrabenazine) is a vesicular monoamine transporter (VMAT2) inhibtior with an Ki value of 0.97 nM.
  24. IBAT inhibitor

    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ?? 0.17 nM, 0.13 ?? 0.03 nM, and 5.8 ?? 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  25. 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.
  26. ROMK inhibitor

    MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
  27. Sunifiram (DM-235) is a piperazine derived ampakine-like drug which has nootropic effects in animal studies with significantly higher potency than piracetam.
  28. 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.
  29. URAT1 inhibitor

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

    Nav1.7 inhibitor is a potent Nav1.7 inhibitor.
  31. 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.
  32. calcium channel inhibitor

    Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM).
  33. 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).
  34. calcium-sensing receptor (CaR) antagonist

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

    Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
  36. 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.
  37. 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.
  38. 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.
  39. P-glycoprotein inhibitor

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

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

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

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

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

  45. Sodium Channel Nav1.7 inhibitor

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

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

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

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

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

    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.

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