Gestrinone

CAS No. 16320-04-0

Gestrinone( R 2323 )

Catalog No. M20652 CAS No. 16320-04-0

Gestrinone is a synthetic androgen receptor agonist and ER and progesterone receptor antagonist used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Gestrinone
  • Note
    Research use only, not for human use.
  • Brief Description
    Gestrinone is a synthetic androgen receptor agonist and ER and progesterone receptor antagonist used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
  • Description
    Gestrinone is a synthetic androgen receptor agonist and ER and progesterone receptor antagonist used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.(In Vitro):Gestrinone binds to endometrial receptors for estrogen, progesterone and androgen, occupies all specific binding sites of steroids in the steroid target cells despite the presence of endogenous steroids. Gestrinone exhibits stronger inhibitory effects on the growth of leiomyoma cells at 60 h than that at 20 and 40 h. Leiomyoma cells appears less dense, the cytoplasm is atrophic, the intercellular connections dwindled and nuclear aggregations are observed with more than 10 μM gestrinone treatment. Gestrinone treatment reduces the relative mRNA levels of estrogen α in a concentration dependent manner at concentrations of 0.1-3.0 μM.(In Vivo):The estrogen-sensitive endpoints, vaginal keratinization and uterine progesterone receptor concentration, are enhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicate that danazol and gestrinone have estrogenic activity that is masked by the androgenic component of these drugs. The mean hormone binding globulin treated with gestrinone fell from 56.4 nM to 28.1 nM after one week’s treatment and to 7.1 nM after 4 weeks respectively.
  • In Vitro
    Gestrinone binds to endometrial receptors for estrogen, progesterone and androgen, occupies all specific binding sites of steroids in the steroid target cells despite the presence of endogenous steroids. Gestrinone exhibits stronger inhibitory effects on the growth of leiomyoma cells at 60 h than that at 20 and 40 h. Leiomyoma cells appears less dense, the cytoplasm is atrophic, the intercellular connections dwindled and nuclear aggregations are observed with more than 10 μM gestrinone treatment. Gestrinone treatment reduces the relative mRNA levels of estrogen α in a concentration dependent manner at concentrations of 0.1-3.0 μM.
  • In Vivo
    The estrogen-sensitive endpoints, vaginal keratinization and uterine progesterone receptor concentration, are enhanced by treatment with a combination of flutamide and either danazol or gestrinone. These data indicate that danazol and gestrinone have estrogenic activity that is masked by the androgenic component of these drugs. The mean hormone binding globulin treated with gestrinone fell from 56.4 nM to 28.1 nM after one week’s treatment and to 7.1 nM after 4 weeks respectively.
  • Synonyms
    R 2323
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    ER
  • Research Area
    Others
  • Indication
    Endometriosis with or without accompanying sterility

Chemical Information

  • CAS Number
    16320-04-0
  • Formula Weight
    308.41
  • Molecular Formula
    C21H24O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:50 mg/mL (162.12 mM)
  • SMILES
    [H][C@@]12CC[C@@](O)(C#C)[C@@]1(CC)C=CC1=C3CCC(=O)C=C3CC[C@@]21[H]
  • Chemical Name
    (8S13S14S17S)-13-ethyl-17-ethynyl-17-hydroxy-126781314151617-decahydro-3H-cyclopenta[a]phenanthren-3-one

Shipping & Storage Information

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

Reference

1.Hui-Ling X Ning Y Jing W et al. Therapeutic effects of mifepristone combined withGestrinone on patients with endometriosis[J]. Pakistan Journal of Medical Sciences 2016 32(5).
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