GR3027

CAS No. 2089238-18-4

GR3027( GR-3027 | Golexanolone )

Catalog No. M13263 CAS No. 2089238-18-4

GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GR3027
  • Note
    Research use only, not for human use.
  • Brief Description
    GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.
  • Description
    GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC; inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor; during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor; restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy.Sleep Disorder Phase 2 Clinical.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    GR-3027 | Golexanolone
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    GAT
  • Recptor
    GAT
  • Research Area
    Neurological Disease
  • Indication
    Sleep Disorder

Chemical Information

  • CAS Number
    2089238-18-4
  • Formula Weight
    329.484
  • Molecular Formula
    C21H31NO2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    C[C@]1([C@](CC/2)([H])[C@]3([H])CC[C@@]4([H])C[C@](O)(C#C)CC[C@]4(C)[C@@]3([H])CC1)C2=N\O
  • Chemical Name
    (17E)-3α-ethynyl-17-(hydroxyimino)-5α-androstan-3β-ol

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Johansson M, et al. Am J Physiol Gastrointest Liver Physiol. 2015 Sep 1;309(5):G400-9. 2. Johansson M, et al. J Steroid Biochem Mol Biol. 2016 Jun;160:98-105. 3. Johansson M, et al. Psychopharmacology (Berl). 2018 May;235(5):1533-1543. 4. Patent WO 2008/063128.
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