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Rosiglitazone

A Blocker of Kir6.1, KV4.3, TRPM3 and an Activator of TRPC5 and PPAR Ligand
Cat #: R-125
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 357.43
    Purity: >97%
    Form Lyophilized powder.
    Effective concentration 2-200 µM.
    Structure
    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.
    References-Activity
    1. Jeong, I. et al. (2011) Br. J. Pharmacol. 163, 510.
    2. Yu. L. et al. (2011) Br. J. Pharmacol. 164, 2064.
    3. 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.
    Our bioassay
    • Alomone Labs Rosiglitazone inhibits KV4.2 channels expressed in Xenopus oocytes
      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.
    Scientific background 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: 22/09/2020

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

    For research purposes only, not for human use
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