Dienogest Estrogen/progestogen Receptor chemical

Cat.No.S1251

Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.
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Quality Control

Batch: Purity: 99.91%
99.91

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (199.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 311.42 Formula

C20H25NO2

Storage (From the date of receipt)
CAS No. 65928-58-7 Download SDF Storage of Stock Solutions

Synonyms STS 557 SMILES CC12CCC3=C4CCC(=O)C=C4CCC3C1CCC2(CC#N)O

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Mechanism of Action

Targets/IC50/Ki
progestogen Receptor
In vitro
Dienogest activates progesterone receptor (EC50=3.4 or 10.5 nM) with antagonistic activity on androgen receptor (EC50=420.6 or 775.0 nM) but not agonistic nor antagonistic action on GR, MR (3000 nM). This compound combined with Oestradiol leads to an increase in the levels of prolactin mRNA and prolactin production in a dose-dependent manner in human endometrial stromal cells (ESC). It directly acts on endometrial tissue in progestogenic response, such as decidualization, increases prolactin production and growth retardation. This chemical at concentration of 0.1 μM and 1 μM significantly inhibits BrdU incorporation into DNA at 24 and 48 hours in the cultured endometriotic stromal cells. It significantly increases the cells in G0/G1 phase and reduces the cells in S phase and G2/M phase in 24 and 48 hours in the cultured endometriotic stromal cells.
In vivo
Dienogest (0.1-1 mg/kg per day, p.o.) reduces the endometrial implant volume to the same extent as Danazol (100 mg/kg per day, p.o.) in rats. This compound ameliorates the endometrial implant-induced alterations of the immune system: i.e. it increases the natural killer activity of peritoneal fluid cells and splenic cells, decreases the number of peritoneal fluid cells, and decreases interleukin-1beta production by peritoneal macrophages. It (0.1 mg/kg per day) combined with Buserelin (0.3 mg/kg per day) suppresses the bone mineral loss induced by buserelin alone, with no reduction of the effect on endometrial implants.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9506869/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-09-18)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07164183 RECRUITING
Endometriosis
Alcea
2025-09-11 PHASE3
NCT07770594 COMPLETED
Endometrioma
Mst.Sumyara Khatun
2025-04-17
NCT05697471 UNKNOWN
Endometriosis
Far Eastern Memorial Hospital
2023-02-25 PHASE3
NCT06543550 UNKNOWN
Endometriosis
Bio Meds Pharmaceutica Ltda
2024-07-30 PHASE4
NCT06719934 NOT_YET_RECRUITING
Adenomyosis
Al-Azhar University
2025-01-01 PHASE1
NCT05937490 UNKNOWN
Adenomyosis
Azienda Ospedaliero-Universitaria di Modena
2023-03-27 PHASE4

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