Dienogest是一种孕酮受体激动剂，作用于子宫内膜异位，有口服的子宫内膜活性。

Dienogest 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.

Dienogest（0.1 mg/kg/day）和乙基酰胺（0.3 mg/kg/day）联用可抑制乙基酰胺诱发,且不影响对子宫内膜植入物的效果.Dienogest（0.1-1 mg/kg/day,p.o.）使大鼠子宫内膜植入体体积降低,程度和达那唑（100 mg/kg/day,p.o.）相同.

在培养的子宫内膜异位的基质细胞中, Dienogest（0.1-1 μM）在24和48 h后对BrdU掺入到DNA中有显著抑制作用,还明显增加处于G0/ G1期的细胞,并使处于S期和G2 / M期的细胞减少。Dienogest激活孕激素受体（EC50：3.4/10.5 nM）；对雄激素受体有拮抗作用（EC50：420.6/775.0 nM）,但对GR和MR没有拮抗作用（3 nM）。在人子宫内膜基质细胞中,Dienogest和雌（甾）二醇联用可剂量依赖地增加催乳素mRNA和蛋白水平。

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).

65928-58-7

C20H25NO2

311.425

STS 557;地诺孕素

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:58 mg/mL (186.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years