Membrane Transporters-Ion Channels

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  1. Calcium channel blocker

    Efonidipine is a dihydropyridine calcium channel blocker that blocks both T-type and L-type calcium channels. It has also been studied in atherosclerosis and acute renal failure.
  2. Potassium channel blocker

    Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk.
  3. TRPM4 blocker

    Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model.
  4. Calcium channel blockers

    Nicardipine(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.
  5. Calcium channel blocker

    Fendiline hydrochloride is a nonselective calcium channel blocker.
  6. Calcium channel blocker

    Lercanidipine is a calcium channel blocker of the dihydropyridine class, which works by relaxing and opening the blood vessels allowing the blood to circulate more freely around the body. This lowers the blood pressure and allows the heart to work more efficiently.
  7. potassium-competitive acid blocker

    Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM.
  8. calcium channel blocker

    Bepridil hydrochloride (CERM 1978) is a calcium channel blocker, with antianginal activity.
  9. dual T-type and L-type calcium channel blocker

    Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a dual T-type and L-type calcium channel blocker (CCB).
  10. Kir7.1 potassium channels blocker

    ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
  11. Nav1.7/Nav1.8 blocker

    DSP-2230 is a selective Nav1.7/Nav1.8 blocker.
  12. potassium channel blocker

    VU0134992 is a selective inward rectifier potassium (Kir) channel Kir4.1 blocker with an IC50 of 0.97 ?M.
  13. NaV1.8 blocker

    PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
  14. Sodium channel blocker

    Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.
  15. Cav 2.2 blocker

    Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC50 of 1 nM.
  16. NaV1.8 blocker

    PF 04531083 is a selective NaV1.8 blocker, and used for the research of neuropathic/inflammatory pain.
  17. VSCC blocker

    PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
  18. NAADP antagonist and TPC blocker

    trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
  19. CatSper channels blocker

    HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 ?M).
  20. calcium channel blocker

    ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
  21. benzazepine calcium channel blocker

    SQ-31765 is a benzazepine calcium channel blocker.
  22. calcium channel blocker

    Tiapamil hydrochloride is a calcium channel blocker.
  23. sAHP channel blocker

    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization.
  24. KV7 channel blocker

    DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
  25. Kv7 (KCNQ) channels blocker

    XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 ?M, 0.71 ?M, 0.6 μM, and 0.98 ?M, respectively.
  26. potassium channel blocker

    Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current.
  27. lipophilic calcium channel blocker

    Teludipine is a lipophilic calcium channel blocker.
  28. IKs blocker

    HMR 1556, a chromanol derivative, is a IKs blocker with IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively.
  29. Na+ blocker

    Ralfinamide (FCE-26742A) is an orally available Na+ blocker derived from α-aminoamide, with function of suppressing pain.
  30. sodium channel blocker

    Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.
  31. Ca2+ Channel Blocker

    NS-638 is a small nonpeptide molecule with Ca2+-channel blocking properties. K+-stimulated intracellular Ca2+-elevation is blocked with an IC50 value of 3.4 μM.
  32. IK blocker

    AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK).
  33. intravenous BKCa-channel blocker

    GAL-021 a new intravenous BKCa-channel blocker.
  34. 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.
  35. NaV1.7 blocker

    XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.
  36. AMPA receptor blocker

    gamma-DGG is a competitive AMPA receptor blocker.
  37. HCN channel blocker

    ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
  38. 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.
  39. non-voltage dependent calcium channel blocker

    Carboxyamidotriazole (L 651582) is a blocker of non-voltage dependent calcium channel.
  40. IKs blocker

    JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
  41. 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.
  42. 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).
  43. 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.
  44. 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.
  45. Na+ channel blocker

    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
  46. sodium channel blocker

    Levobupivacaine hydrochloride is a sodium channel blocker.
  47. 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.
  48. TRPM8 channel blocker

    TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells
  49. Calcium channel blocker

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

  50. 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. 

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