地诺孕素 T2577

Product Introduction
Bioactivity


英文名: Dienogest

描述: Dienogest (STS 557) 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。

激酶实验: 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).

体外活性: 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.

体内活性: 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。

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 58 mg/mL (186.2 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: COX-2 | Progesterone Receptor | menorrhagia | Inhibitor | Dienogest | PGE2 | inhibit | EM-PR cells | NR3C3 | STS557 | STS-557 | endometriosis | menopause

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相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Endocrinology-Hormone Compound Library | Bioactive Compound Library

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