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Oroxylin A

6-Methoxybaicalein, 5,7-Dihydroxy-6-methoxyflavone
An Antagonist of GABA(A) Receptors
    Cat #: O-160
    Alternative Name 6-Methoxybaicalein, 5,7-Dihydroxy-6-methoxyflavone
  • Lyophilized Powder
  • Bioassay Tested
    • Origin Scutellaria baicalensis.
    Source Natural
    MW: 284.26
    Purity: >98% (HPLC)
    Effective concentration 10 nM – 10 µM.
      • Oroxylin A
    Chemical name 5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one.
    Molecular formula C16H12O5.
    CAS No.: 480-11-5.
    PubChem CID 5320315
    Activity A flavonoid antagonist at the benzodiazepine site of the GABAA receptors. Inhibits [3H]Flunitrazepam binding to rat cerebral cortical membranes (IC50 = 1.09 µM), and selectively abolishes the anxiolytic, myorelaxant and motor incoordination, but not the sedative and anticonvulsant effects elicited by diazepam in mice1.
      • Huen, M.S. et al. (2003) Biochem. Pharmacol. 66, 125.
    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 4°C. Keep in a tightly sealed container to protect from air. Protect from light.
    Solubility Up to 50 mM in DMSO. Centrifuge all products before reconstitution (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C. It is recommended to aliquot reconstituted product for storage.
      • Oroxylin A
        Alomone Labs Oroxylin A inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
        Percent inhibition of the specific binding of 1 nM [3H]Flunitrazepam to membranes from whole rat brain (except cerebellum) was plotted against concentrations of Oroxylin A (#O-160), (green circles) and of Diazepam (assay standard, black squares) and used to calculate IC50 and Ki values for Oroxylin A (IC50 ≈ 1.19 μM, and Ki ≈ 0.97 μM).
    References - Scientific background

      • Oroxylin A, also called 6-Methoxybaicalein, is an antagonist at the benzodiazepine site of the GABA(A) receptors.

        Oroxylin A is an active O-methylated flavone compound that was originally isolated from the medicinal plant Scutellaria baicalensis. Oroxylin A was shown to have multiple functions, including anti-inflammatory, anti-cancer and anti-thrombotic activities. In addition, it has dopamine reuptake inhibitor activity and an inhibitory effect on nuclear factor-κB activation. The compound was used to treat pulmonary infection in Korea, China, and Japan1,2.

        GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter, through the central nervous system. The GABAA receptor is considered to be a major target of antiseizure drugs3.

    Target GABA(A) receptors
    Lyophilized Powder
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    Last update: 21/07/2019

    Oroxylin A (#O-160) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use
    Citations
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