16320-04-0
16320-04-0 structure
- Name: Gestrinone
- Chemical Name: Gestrinone
- CAS Number: 16320-04-0
- Molecular Formula: C21H24O2
- Molecular Weight: 308.414
- Catalog: API Hormone and endocrine-regulating drugs Birth control pills
- Create Date: 2018-05-27 08:00:00
- Modify Date: 2024-01-14 15:49:59
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Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
| Name | Gestrinone |
|---|---|
| Synonyms |
D-GESTRINONE
Dimetriose TridoMose 13b-Ethyl-17a-ethynyl-D4,9,11-gonatriene-17b-ol-3-one (17a)-13-Ethyl-17-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one 13b-Ethyl-17a-ethynyl-17b-hydroxy-4,9,11-gonatrien-3-one Dimetrose MFCD00865561 gestrigone (17α)-13-Ethyl-17-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one 18,19-Dinorpregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-, (17α)- Gestrinone (8S,13S,14S,17R)-13-Ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,13,14,15,16,17-decahydro-3H-cyclopenta[a]phenanthren-3-one 13-ETHYL-17α-ETHYNYL-17β-HYDROXY-4,9,11-GONATRIENE-3-ONE NeMestran |
| Description | Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM. |
|---|---|
| Related Catalog | |
| 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]. |
| Cell Assay | 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]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 507.6±50.0 °C at 760 mmHg |
| Melting Point | 154ºC |
| Molecular Formula | C21H24O2 |
| Molecular Weight | 308.414 |
| Flash Point | 214.9±22.7 °C |
| Exact Mass | 308.177643 |
| PSA | 37.30000 |
| LogP | 3.27 |
| Vapour Pressure | 0.0±3.0 mmHg at 25°C |
| Index of Refraction | 1.607 |
| Storage condition | -20°C Freezer |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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| Precursor 0 | |
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| DownStream 1 | |
