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: 65928-58-7

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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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
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 lnformation & 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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