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Ganaxolone

CCD-1042, 3α-Hydroxy-3β-methyl-5α-pregnan-20-one, AC1OCF9O, UNII-98WI44OHIQ
A Selective Positive Modulator of GABA(A) Receptors
    Cat #: G-120
    Alternative Name CCD-1042, 3α-Hydroxy-3β-methyl-5α-pregnan-20-one, AC1OCF9O, UNII-98WI44OHIQ
  • Lyophilized Powder
  • Bioassay Tested
    • Source Synthetic
    MW: 332.5
    Purity: ≥99%
    Effective concentration 0.01-10 μM.
    Structure
    • Ganaxolone
    Chemical name 1-[(3R,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-3,10,13-trimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]ethanone.
    Molecular formula C22H36O2.
    CAS No.: 38398-32-2.
    PubChem CID 6918305
    Activity Ganaxolone potentiates GABA-evoked chloride currents. In Xenopus oocytes expressing the human GABA(A) receptor subunits α2β1γ2L, α3β1γ2L and α1β1γ2L the respective EC50 values are 94, 122 and 213 nM1. It is also used as an anticonvulsant, antiepileptic drug2.
    References-Activity
    1. Carter, R.B. et. al. (1997) J. Pharmacol. Exp. Ther. 280, 1284.
    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 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Ganaxolone
      Alomone Labs Ganaxolone inhibits specific binding of TBPS to rat brain cortex GABA(A) receptors.
      Percent inhibition of specific binding of 2 nM [35S] TBPS to membranes from rat brain cerebral cortex was plotted against concentrations of Ganaxolone (#G-120), (green circles) and of Picrotoxin (assay standard, black squares) and used to calculate IC50 and Ki values for Ganaxolone (IC50 ≈ 0.81 µM, and Ki ≈ 0.79 µM).
    References - Scientific background
    1. Carter, R.B. et. al. (1997) J. Pharmacol. Exp. Ther. 280, 1284.
    2. Nohria, V. and Giller, E. (2007) Neurotherapeutics 4, 102.
    3. Reddy, D.S. and Rogawski, M.A. (2010) Epilepsy Res. 89, 254.
    Scientific background

    Ganaxolone (CCD 1042) is a 3β-methyl-substituted synthetic analogue of the endogenous neuroactive steroid allopregnanolone with anticonvulsant, anxiolytic, and sedative effects. The methyl group on the compound makes it more resistant to metabolism and increases the compound’s half life by hours.

    Ganaxolone is a selective, potent and positive allosteric modulator of the GABA(A) receptors. It enhances the binding of the benzodiazepine and the GABA sites. In several clinical studies, ganaxolone treatment showed to have protective activity in several seizures models in adults and in children with history of infantile spasms. In adults the compound successfully reduced the frequency of partial seizures2,3.

    Ionotropic GABA(A) receptors mediate GABA action, a major inhibitory neurotransmitter, through the central nervous system. The receptors are considered to be a major target of antiseizure drugs1,2.

    Target GABA(A) receptors
    Lyophilized Powder
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    Last update: 24/01/2020

    Ganaxolone (#G-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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