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Dienogest

Catalog No. T2577 CAS 65928-58-7

Synonyms: STS 557

Dienogest (STS 557) is an orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive.

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Dienogest, CAS 65928-58-7

Pack Size	Availability	Price/USD
10 mg	In stock	$ 46.00
25 mg	In stock	$ 61.00
50 mg	In stock	$ 77.00
100 mg	In stock	$ 126.00
200 mg	In stock	$ 163.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.89%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Dienogest (STS 557) is an orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive.
In vitro	Concurrent administration of Dienogest (0.1 mg/kg/day) and Ethinyl estradiol (0.3 mg/kg/day) can inhibit the effects induced by Ethinyl estradiol without affecting the efficacy on uterine endometrial implants. Additionally, Dienogest administered orally at doses ranging from 0.1 to 1 mg/kg/day reduces the volume of endometrial implants in rats, achieving a reduction similar to that of Danazol at 100 mg/kg/day, also administered orally.
In vivo	In cultured endometriotic stromal cells, Dienogest (0.1-1 μM) significantly inhibits BrdU incorporation into DNA after 24 and 48 hours, also notably increases the number of cells in the G0/G1 phase while decreasing the cells in the S and G2/M phases. Dienogest activates progesterone receptors (EC50: 3.4/10.5 nM) and antagonizes androgen receptors (EC50: 420.6/775.0 nM) without exhibiting antagonism towards GR and MR at 3 nM. In human endometrial stromal cells, the combined use of Dienogest and estradiol (estrogen) dose-dependently increases prolactin mRNA and protein levels.
Kinase Assay	Kinase inhibition assays: For the VEGFR2, Flk1 and FGFR1 kinase assays, BMS-582664 is dissolved in DMSO and diluted with water/10% DMSO to a final DMSO concentration of 2%. The kinase reactions consists of 8 ng of enzymes with GST tag, 75 μg/mL substrate, 1 μM ATP, and 0.04 μCi [γ-33P]ATP in 50 μL total reaction volume (kinase buffer:? 20 mM Tris, pH 7.0, 25 μg/mL BSA, 1.5 mM MnCl2, 0.5 mM dithiothreitol). In all cases, the reactions are incubated for 60 min at 27℃ and terminated with the addition of cold trichloroacetic acid (TCA) to a final concentration of 15%. The percent inhibition from the kinase assays is determined by nonlinear regression analyses, and data are reported as the inhibitory concentration required to achieve 50% inhibition relative to control reactions (IC50).

Synonyms	STS 557
Molecular Weight	311.42
Formula	C20H25NO2
CAS No.	65928-58-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 58 mg/mL (186.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Sasagawa S, et al. Steroids, 2008, 73(2), 222-231. 2. Okada H, et al. Mol Hum Reprod, 2001, 7(4), 341-347. 3. Fu L, et al. Fertil Steril, 2008, 89(5 Suppl), 1344-1347. 4. Katsuki Y, et al. Eur J Endocrinol, 1998, 138(2), 216-226.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Nuclear Receptor Compound Library Bioactive Compound Library Approved Drug Library Bioactive Compounds Library Max Clinical Compound Library Apoptosis Compound Library

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Keywords

Dienogest 65928-58-7 Apoptosis Autophagy Endocrinology/Hormones Others Estrogen/progestogen Receptor Progesterone Receptor COX-2 menorrhagia Inhibitor PGE2 inhibit STS 557 EM-PR cells NR3C3 STS557 STS-557 endometriosis menopause inhibitor

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