Home Endocrinology & Hormones Estrogen/progestogen Receptor chemical Dienogest For research use only.

Dienogest

Synonyms: STS 557

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

Dienogest Chemical Structure

Dienogest Chemical Structure

CAS No. 65928-58-7

Purity & Quality Control

Dienogest Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04808843 Active not recruiting
Endometriosis Associated Pelvic Pain
Bayer
 May 13 2022 --
NCT04901377 Completed
Oral Contraception
Bayer
 June 24 2021 --
NCT05272930 Completed
Fibromyalgia|Endometriosis Ovary|Dienogest
Gaziosmanpasa Research and Education Hospital
 June 30 2021 --

Chemical Information & Solubility

Molecular Weight 311.42 Formula

C20H25NO2
CAS No. 65928-58-7 SDF Download Dienogest SDF
Smiles CC12CCC3=C4CCC(=O)C=C4CCC3C1CCC2(CC#N)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (199.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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