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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 yes
  • Bioassay Tested
    • Origin Scutellaria baicalensis.
    Source Natural
    MW: 284.26
    Purity: >98% (HPLC)
    Effective concentration 10 nM – 10 µM.
    Structure
    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.
    References-Activity
    1. 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.
    Our bioassay
    • Alomone Labs Oroxylin A inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
      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
    1. Lee, J.Y. and Park, W. (2016) Exp. Ther. Med. 12, 151.
    2. Kwon, B.E. et al. (2016) PLoS One 11, 5.
    3. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    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
    Last update: 12/08/2021

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

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    For research purposes only, not for human use
    Shipping and Ordering information

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