Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 255 | 现货 | ||
10 mg | ¥ 415 | 现货 | ||
50 mg | ¥ 758 | 现货 | ||
100 mg | ¥ 1,246 | 现货 | ||
200 mg | ¥ 1,617 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 457 | 现货 |
产品描述 | 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. |
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。 |
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). |
别名 | 地诺孕素, STS 557 |
分子量 | 311.42 |
分子式 | C20H25NO2 |
CAS No. | 65928-58-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 58 mg/mL (186.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2111 mL | 16.0555 mL | 32.111 mL | 80.2774 mL |
5 mM | 0.6422 mL | 3.2111 mL | 6.4222 mL | 16.0555 mL | |
10 mM | 0.3211 mL | 1.6055 mL | 3.2111 mL | 8.0277 mL | |
20 mM | 0.1606 mL | 0.8028 mL | 1.6055 mL | 4.0139 mL | |
50 mM | 0.0642 mL | 0.3211 mL | 0.6422 mL | 1.6055 mL | |
100 mM | 0.0321 mL | 0.1606 mL | 0.3211 mL | 0.8028 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Dienogest 65928-58-7 Apoptosis Autophagy Endocrinology/Hormones Others Estrogen/progestogen Receptor Progesterone Receptor COX-2 地诺孕素 menorrhagia Inhibitor PGE2 inhibit STS 557 EM-PR cells NR3C3 STS557 STS-557 endometriosis menopause inhibitor