Dienogest

Catalog No.S1251 Batch:S125103

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Technical Data

Formula

C20H25NO2
Molecular Weight 311.42 CAS No. 65928-58-7
Solubility (25°C)* In vitro DMSO 62 mg/mL (199.08 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.