Home Endocrinology & Hormones Estrogen/progestogen Receptor chemical Dienogest

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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.
Dienogest Estrogen/progestogen Receptor chemical Chemical Structure

Chemical Structure

Molecular Weight: 311.42

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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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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.

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Mechanism of Action

Targets/IC50/Ki
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] 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. [2] 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. [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. 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. [4]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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 --

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