Dienogest

Catalog No.S1251 Synonyms: STS 557

For research use only.

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

Dienogest Chemical Structure

CAS No. 65928-58-7

Purity & Quality Control

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Biological Activity

Description Dienogest (STS 557) is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.
Targets
progestogen Receptor [1]
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). [1] Dienogest 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). Dienogest directly acts on endometrial tissue in progestogenic response, such as decidualization, increases prolactin production and growth retardation. [2] Dienogest 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. Dienogest 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. [3]

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. Dienogest 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. Dienogest (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. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 62 mg/mL
(199.08 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 311.42
Formula

C20H25NO2

CAS No. 65928-58-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12CCC3=C4CCC(=O)C=C4CCC3C1CCC2(CC#N)O

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

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04808843 Not yet recruiting Drug: Dienogest (BAY86-5258 Visanne) Endometriosis Bayer August 31 2021 --
NCT04901377 Recruiting Combination Product: Estradiol valerate/ Dienogest Oral Contraceptive Bayer June 24 2021 --
NCT02728245 Withdrawn Drug: Dienogest|Drug: Placebo drug|Procedure: Surgery Ovarian Reserve|Endometriosis Seoul National University Hospital|Kyung Hee University Hospital at Gangdong|Korea University Guro Hospital|Ajou University School of Medicine|Ewha Womans University Mokdong Hospital|Asan Medical Center October 2017 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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