Rosiglitazone

A Blocker of Kir6.1, KV4.3, TRPM3 and an Activator of TRPC5 and PPAR Ligand
    Cat #: R-125
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 357.43
    Purity: >97%
    Form Lyophilized powder.
    Effective concentration 2-200 µM.
      • Rosiglitazone
    Chemical name 5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione Rosiglitazone.
    Molecular formula C18H19N3O3S.
    CAS No.: 122320-73-4.
    Activity Rosiglitazone blocks KV4.3 channels with an IC50 = 24.5 μM1, Kir6.1 channels with as IC50 = 2 μM2 and blocks TRPM3 channels with IC50 = 5-10 μM3. At high concentrations Rosiglitazone activates TRPC5 channels3.
      • Jeong, I. et al. (2011) Br. J. Pharmacol. 163, 510.
      • Yu. L. et al. (2011) Br. J. Pharmacol. 164, 2064.
      • Majeed, Y. et al. (2011) Mol. Pharmacol. 79, 1023.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in DMSO . Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
      • Rosiglitazone
        Alomone Labs Rosiglitazone inhibits KV4.2 channels expressed in Xenopus oocytes
        A. Time course of KV4.2 peak current amplitude, elicited by 100 ms voltage step from holding potential of -100mV to 0mV, delivered every 10 seconds. Application of 100 µM Rosiglitazone (#R-125) blocks the KV4.2 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 100 µM Rosiglitazone as indicated.
    References - Scientific background
    • 1. Corona, J.C. et al. (2013Exp. Neurol253, 16.
    • 2. Jeong, I. et al. (2011) Br. J. Pharmacol. 163, 510.
    • 3. Yu. L. et al. (2011) Br. J. Pharmacol. 164, 2064.
    • 4. Majeed, Y. et al. (2011) Mol. Pharmacol. 79, 1023.
      • Rosiglitazone is known to activate Peroxisome proliferator-activated receptors (PPAR), ligand-activated transcription factors that belong to the nuclear hormone receptor superfamily1. Data shows that Rosiglitazone blocks KV4.3 channels with an IC50 = 24.5 μM2, Kir6.1 channels with as IC50 = 2 μM3 and blocks TRPM3 channels with IC50 = 5-10 μM4. At high concentrations Rosiglitazone activates TRPC5 channels4.
    Target KV4, Kir6.1, TRPM3, TRPC5 channels
    Last update: 24/01/2020

    Rosiglitazone (#R-125) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use