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Gestrinone (Synonyms: R 2323)

Cat. No.: HY-101405 Purity: 99.87%
Handling Instructions

Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.

For research use only. We do not sell to patients.

Gestrinone Chemical Structure

Gestrinone Chemical Structure

CAS No. : 16320-04-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
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Description

Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.

IC50 & Target

IC50: 43.67 μM (leiomyoma cells)[2]

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[1]. 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[2].

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[3]. 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[4].

Molecular Weight

308.41

Formula

C₂₁H₂₄O₂

CAS No.

16320-04-0

SMILES

C#C[[email protected]]1(O)CC[[email protected]@]2([H])[[email protected]]3([H])CCC4=CC(CCC4=C3C=C[[email protected]]12CC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (162.12 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2424 mL 16.2122 mL 32.4244 mL
5 mM 0.6485 mL 3.2424 mL 6.4849 mL
10 mM 0.3242 mL 1.6212 mL 3.2424 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Gestrinone is dissolved in DMSO and diluted in cell culture media. The final concentration of DMSO in the culture media is 0.5%. The cells are cultured in 96-well plates and treated with DMSO or graded concentrations of gestrinone (0.1, 0.5, 1.0, 5.0, 10, 50 or 100 μM) for 20, 40 and 60 h. The absorbance (OD) at 450 nm is read to determine the cell viability in each well[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.87%

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Keywords:

GestrinoneR 2323R2323R-2323Estrogen Receptor/ERRInhibitorinhibitorinhibit

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Gestrinone
Cat. No.:
HY-101405
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