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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Endocrinology & Hormones>Estrogen / progestogen Receptor Chemical>Dienogest
Dienogest
  • Dienogest

Dienogest NEW

Price $46 $77 $126
Package 10mg 50mg 100mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Dienogest CAS No.: 65928-58-7
Purity: 99.89% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameDienogest
DescriptionDienogest (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.
Kinase AssayKinase 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).
In vitroConcurrent 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 vivoIn 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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (192.67 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsCOX-2 | Progesterone Receptor | menorrhagia | Inhibitor | Dienogest | PGE2 | inhibit | EM-PR cells | NR3C3 | STS557 | STS-557 | endometriosis | menopause
Inhibitors RelatedStavudine | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Tributyrin | Paeonol | Naringin
Related Compound LibrariesBioactive Compound Library | Pediatric Drug Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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