Dienogest

SKU: orb1305303

Description

Dienogest (STS 557) is a fourth-generation, non-ethinylated progestin with oral activity, exhibiting antiproliferative, antiandrogenic, anti-inflammatory, and antiangiogenic properties. It is utilized in hormone therapy and contraception, and is widely applied in preclinical research for studying endometriosis and related gynecological disorders in both in vitro and in vivo models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 65928-58-7
• MW: 311.42
• Purity: 99.89% (May vary between batches)
• Formula: C₂₀H₂₅NO₂
• SMILES: CC12CCC3=C4CCC(=O)C=C4CCC3C1CCC2(O)CC#N
• Target: Apoptosis,Autophagy,Estrogen/progestogen Receptor,Progesterone Receptor
• Solubility: DMSO:60 mg/mL (192.67 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.42 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, EstrogenReceptor, Estrogen Receptor, endometriosis, EM-PR cells, ER, menopause, menorrhagia, NR3C3, inhibit, COX-2, Dienogest, Apoptosis, Autophagy, STS 557, STS557, STS-557, ProgesteroneReceptor, Progesterone Receptor, progestogen Receptor, progestogenReceptor, PGE2

Compound Identifiers

PubChem CID

13175121