Dexamethasone

地塞米松,氟美松,DHAP

Dexamethasone (DEX), a synthetic glucocorticoid, is widely used in clinical settings for its anti-inflammatory effect. Dexamethasone (DHAP)是一种抗炎剂和免疫抑制剂。

目录号
EY0013
EY0013
纯度
99.19%
99.19%
规格
50 mg
100 mg
原价
598.00_
900
售价
598.00_
900
库存
现货
现货
订购
订购
订购
订购
订购
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  • 生物活性

    An anti-inflammatory glucocorticoid. Inhibits the expression of the inducible but not the constitutive nitric oxide synthase in vascular endothelial cells (IC₅₀ = 5 nM). Enhances active cation transport in aortic smooth muscle cells by stimulating the Na+-K+ pump. Has anti-inflammatory and anti-rheumatic properties. Induces apoptosis in human thymocytes. In general, 500-1000 nM of dexamethasone is sufficient to induce apoptosis following a 6-hour incubation at 37 °C.

     

    Dexamethasone increase ob gene expression with a EC50 of 10nM.[8]

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

    CA enzyme activity assay[9]

    The activity of CA isozymes can be assayed by esterase activity that can be performed in vitro and followed spectrophotometrically at 348 nm. 4-nitrophenyl acetate (NPA) is the substrate in this method. We screened the conversion from 4-nitrophenyl acetate (NPA) to 4-nitrophenylate over a period of 3 min at 25 °C in the spectrophotometer. The enzymatic reaction contained 50 mM Tris–SO4 buffer (pH = 7. 4), 3 mM 4-nitrophenyl acetate, and enzyme solution in a total volume of 1 mL. A reference measurement was taken by the same cuvette without enzyme solution. The inhibitory effects of tenoxicam, fluorometholone acetate, and dexamethasone on the activity of purified carbonic anhydrase enzyme from human erythrocyte were tested. These experiments were performed three times for five different drug concentrations.

    Control activity in the absence of drug was ascertained to be 100%. A percent activity versus drug concentration graph was plotted and IC50 values were calculated from these curves. Ki values of the drugs were calculated by measuring enzyme activity at three different drug concentrations with five different substrate concentrations. Ki constant and inhibition type Lineweaver–Burk curves were used.

  • 细胞实验

    Cell proliferation and its suppression[10]

    Whole blood was collected by jugular venipuncture into lithium heparinized tubes and processed within 1 h after collection, in healthy dogs. Density-gradient centrifugation with Histopaque 1077 was done to harvest peripheral blood mononuclear cells (PBMCs). A commercially available

    cell-proliferation dye (CPD), eFluor 670, was used to assess lymphocyte proliferation. This fluorochrome-tagged dye binds to cellular proteins containing primary amines and is distributed equally to daughter cells upon division; thus, as cells divide, fluorescent staining becomes less bright. CPD eFluor 670 was added at concentrations of 5.0 μM to washed PBMCs (5 x 105cells). The cells were incubated for 10 min at 37°C in the dark, and labeling was stopped by the addition of 5 volumes giving (500 mL of cold complete RPMI (cRPMI) medium (RPMI 1640), with 10% fetal bovine serum (FBS), 5 mL of 1-M Hepes, 0.35 L of diluted b-mercaptoethanol, 5 mL of penicillin–streptomycin–glutamine, and 1.1 g of sodium bicarbonate. The cells were washed 3 times with cRPMI and transferred to 96-well platesin the presence of the T-cell mitogen concanavalin A , 5 mg/mL, and increasing concentrations of dexamethasone (0.1, 1, 10, 100, 1000, and 10 000μM). The plates were incubated at 37°C in humidified 5% CO2/95% air for 3 d before the cells were labeled for flow-cytometric analysis.

  • 动物实验

    Animals[11]

    Female nu/nu nude mice (4–5 weeks old, 18–22 g) were obtained. The mice were housed under standard temperature (22–24 °C), humidity (50%–60%) and light (12 h light/12 h dark cycle) conditions with free access to food and water before being used in this study.

    Tumor xenograft model

    A549 cells (1×107cells, suspended in 200 μL of PBS) were inoculated subcutaneously into the right flank of nude mice. At approximately d 7, animals were grouped according to tumor volume, so that all groups had similar starting mean tumor volumes of approximately 100 mm3. The tumor diam­eter was measured with vernier calipers, and tumor volume was calculated by the following formula: tumor volume (mm3)=0.5×A(mm)×B(mm)2, where A is the larger diameter, and B is the smaller diameter.

    Tumor growth inhibition assay

    DEX and TAM(tamoxifen) were dissolved in 10% hydroxypropyl-β-cyclodextrin aqueous solution and 1,2-propanediol, respec­tively. DEX and TAM were administered by intragastric gavage every day. GEM was dissolved in a 0.9% sodium chlo­ride solution and injected intravenously via a tail vein every 3 d. After being randomly divided into different groups with five mice per group, xenograft mice were treated with vehicle solution (as a blank control), TAM (50 mg/kg), GEM (20 mg/kg) and DEX (2, 4 mg/kg). Tumor measurements were taken every two days. After 32 d of treatment, the mice were euthanized by cervical displacement. All tumors and tissues were harvested after the final treatment for later assessment.

     

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Wang F, Yue Z, Xie P, et al. C19-Norditerpenoid Alkaloids from Aconitum szechenyianum and Their Effects on LPS-Activated NO Production. Molecules. 2016;21(9).
    [2] Mateeva N, Gangapuram M, Mazzio E, Eyunni S, Soliman KF, Redda KK. Biological evaluation of synthetic chalcone and flavone derivatives as anti-inflammatory agents. Med Chem Res. 2015;24(4):1672-1680.
    more

    分子式
    C22H29FO5
    分子量
    392.46
    CAS号
    50-02-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    25 mg/mL
    Water
    Insoluble
    Ethanol
    25 mg/mL

    体内溶解度
    约20 mg/mL

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02864602 Anesthesia, Conduction Drug: IV dexamethasone University Health Network, Toronto Phase 3 2016-07-01 2016-08-11
    NCT01255358 Nervous System Disorder|Genetic Syndrome Drug: Dexamethasone Erydel Phase 2 2011-02-01 2011-12-27
    NCT00011362 Infant, Newborn|Infant, Low Birth Weight|Infant, Small for Gestational Age|Infant, Premature|Bronchopulmonary Dysplasia Drug: Dexamethasone Early|Drug: Dexamethasone Late NICHD Neonatal Research Network|National Center for Research Resources (NCRR) Phase 3 1992-09-01 2015-06-03
    NCT01892163 Diabetic Macular Edema Device: Ozurdex Moorfields Eye Hospital NHS Foundation Trust|The Royal Wolverhampton Hospitals NHS Trust|Frimley Park Hospital NHS Trust|Brighton and Sussex University Hospitals NHS Trust|University Hospitals Bristol NHS Foundation Trust Phase 3 2013-03-01 2017-01-03
    NCT02850601 Lichen Planus Drug: Dexamethasone Brigham and Women's Hospital Phase 2 2016-11-01 2016-07-29
    NCT02991339 Liver Dysfunction|Hepatectomy|Bilirubinaemia|Jaundice Drug: Dexamethasone Shanghai Zhongshan Hospital Phase 2|Phase 3 2016-06-01 2016-12-12
    NCT02402725 Multiple Myeloma Drug: Dexamethasone Boston Medical Center Phase 2 2015-05-01 2017-02-14
    NCT01925859 Healthy Drug: EryDex (dexamethasone sodium phosphate encapsulated erythrocytes) Erydel Phase 1 2013-06-01 2015-05-29
    NCT02322242 Shoulder Surgery|Nerve Block Drug: Systemic Dexamethasone|Drug: Perineural dexamethasone Dr. Stephen Choi|The Physicians' Services Incorporated Foundation|Sunnybrook Health Sciences Centre Phase 4 2015-01-01 2017-02-03
    NCT01284478 Pseudophakic Cystoid Macular Edema,|Diabetic Macular Edema Drug: Dexamethasone Implant Northern California Retina Vitreous Associates|Allergan Phase 2 2011-01-01 2012-10-03
    NCT01983449 Peripheral Arterial Diseases Drug: Dexamethasone Sodium Phosphate Injection, USP Mercator MedSystems, Inc. Phase 4 2013-11-01 2017-03-21
    NCT03043495 Dexamethasone|Supraclavicular Brachial Plexus Block Procedure: Ultrasound guided supraclavicular brachial plexus block|Drug: Dexamethasone Eslam Ayman Mohamed Shawki|Cairo University Phase 4 2016-10-01 2017-02-03
    NCT01372904 Cisplatin Ototoxicity Drug: Dexamethasone Phosphate Meir Medical Center Phase 4 2011-06-01 2014-07-16
    NCT03033316 Multiple Myeloma Drug: Dexamethasone Enceladus Pharmaceuticals BV|University Hospital, Aachen|Accelovance Phase 1|Phase 2 2017-01-01 2017-01-24
    NCT02815319 Cancer Drug: Dexamethasone Ottawa Hospital Research Institute Phase 4 2017-01-01 2017-02-21
    NCT01297010 Vomiting Postoperative Drug: Dexamethasone and ondasetron|Drug: Dexamethasone Instituto Materno Infantil Prof. Fernando Figueira|Universidade Federal de Pernambuco Phase 3 2011-03-01 2011-08-02
    NCT01094990 Acute Leukemic Patients in Children Drug: Dexamethasone CHANCHAI TRAIVAREE|Phramongkutklao College of Medicine and Hospital Phase 4 2011-04-01 2012-01-09
    NCT02399657 Diabetes Mellitus|Macular Edema|Retinal Exudates and Deposits Drug: Intravitreal dexamethasone 0.7mg implant Inje University|Allergan Phase 4 2015-02-01 2015-04-02
    NCT01731795 Acute Respiratory Distress Syndrome Drug: Dexamethasone Dr. Negrin University Hospital|Fundacin Mutua Madrilea|Asociacin Cientfica Pulmn y Ventilacin Mecnica Phase 4 2013-04-01 2016-07-12

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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