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Dexamethasone

Dexamethasone

产品编号 T1076   CAS 50-02-2
别名: MK 125, Hexadecadrol, Prednisolone F, NSC 34521, 地塞米松

Dexamethasone 是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。在脂多糖诱导的巨噬细胞炎症反应中,它抑制含有炎性 microRNA-155 的外泌体的产生。

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Dexamethasone, CAS 50-02-2
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其他形式的 Dexamethasone:
产品目录号及名称: Dexamethasone (T1076)
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纯度: 99.91%
纯度: 99.77%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Dexamethasone is a glucocorticoid receptor agonist and an IL receptor modulator.Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses
体外活性 GM-CSF release from A549 cells was inhibited by dexamethasone (EC50 = 2.2 nM). The concentration-dependent ability of dexamethasone (EC50 = 36 nM) to induce transcription of the beta2-receptor was found to correlate with GR DNA binding and occurred at 10-100 fold higher concentrations than the inhibition of GM-CSF release [1]. Following treatment with 1 microM dexamethasone, there was a decrease in transmonolayer paracellular permeability mainly to sucrose, fluorescein, and dextrans of up to 20 KDa [2].
体内活性 Kd values (mean+/-SE) for cortisol in human mononuclear leukocytes (HML) of hypertensive patients were higher than in control subjects (24.6 versus 17.5 nmol/L). Binding capacity (4978 versus 4131 sites/cell), Kd values for dexamethasone (6.7 versus 5.7 nmol/L), and IC50 values for dexamethasone (3.4 versus 3.1 nmol/L) and cortisol (12.2 versus 9.5 nmol/L) were not significantly different [3]. Powerful reduction of neutrophils in bronchoalveolar lavage fluid (BALF) was obtained by a single i.p. injection of dexamethasone (10 mg/kg), whereas treatment with N-acetylcysteine (NAC) only resulted in reduction of neutrophils when administered at a high dose (500 mg/kg). A significant decrease of tumour necrosis factor-alpha, IL-1alpha, IL-1beta IL-6, IL- 12p40, and MIP-1alpha mRNA when mice where treated with dexamethasone but not when treated with NAC [4].
动物实验 NAC was administered at three different doses (10, 100 and 500 mg/kg body weight). At the highest concentration, the acidic pH of the NAC solution was adjusted by adding NaOH. Dexamethasone was administered as a single injection of 1 or 10 mg/kg. Both drugs were dissolved in saline and 400 μl were injected intraperitoneally, either 1 h before or 1 h after LPS exposure. In one experiment, NAC (100 and 500 mg/kg) was injected successively every 4·5 h, starting 1 h before challenge (five injections in total). A control group of LPS-exposed animals were injected intraperitoneally with solvent alone (saline). Intratracheal administration was performed by instillation of 100 μl NAC (50, 100 or 500 mg/kg) or dexamethasone (10 mg/kg) into the lungs of mice anaesthetized with 15 mg/kg Rapinovet (i.v.) [4].
别名 MK 125, Hexadecadrol, Prednisolone F, NSC 34521, 地塞米松
化合物与蛋白结合的复合物

T1076_2

Crystal structure of WT AncGR2-LBD WT bound to dexamethasone and SHP coregulator fragment

分子量 392.46
分子式 C22H29FO5
CAS No. 50-02-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: 6 mg/mL (15.28 mM)

DMSO: 73 mg/mL (186 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Adcock IM, et al. Ligand-induced differentiation of glucocorticoid receptor (GR) trans-repression and transactivation: preferential targetting of NF-kappaB and lack of I-kappaB involvement. Br J Pharmacol. 1999 Jun;127(4):1003-11. 2. Romero IA, et al. Changes in cytoskeletal and tight junctional proteins correlate with decreased permeability induced by dexamethasone in cultured rat brain endothelial cells. Neurosci Lett. 2003 Jun 26;344(2):112-6. 3. Mulatero P, et al. Impaired cortisol binding to glucocorticoid receptors in hypertensive patients. Hypertension. 1997 Nov;30(5):1274-8. 4. Rocksén D, et al. Differential anti-inflammatory and anti-oxidative effects of Dexamethasone and N-acetylcysteine in endotoxin-induced lung inflammation. Clin Exp Immunol. 2000 Nov;122(2):249-56. 5. Ding C, Fu S, Chen X, et al. Epigallocatechin gallate affects the proliferation of human alveolar osteoblasts and periodontal ligament cells, as well as promoting cell differentiation by regulating PI3K/Akt signaling pathway[J]. Odontology. 2021: 1-12. 6. Huang L, Li Q. Notoginsenoside R1 promotes differentiation of human alveolar osteoblasts in inflammatory microenvironment through inhibiting NF‑κB pathway and activating Wnt/β‑catenin pathway[J]. Molecular Medicine Reports. 2020, 22(6): 4754-4762. 7. Zhang, Depeng, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination[J]. Biochemical pharmacology. 2018 Aug;154:183-192. 8. Sun C, Li X, Guo E, et al. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis[J]. Oncogene. 2019: 1-15. 9. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker[J]. . British Journal of Pharmacology. 2021

文献引用

1. Liu Z, Tan S, Zhou L, et al.SCGN deficiency is a risk factor for autism spectrum disorder.Signal Transduction and Targeted Therapy.2023, 8(1): 1-15. 2. Chen S, Zhou X, Li W, et al.Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression.Biochemical Pharmacology.2023: 115800. 3. Xiong W, Jia L, Liang J, et al.Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study.International Immunopharmacology.2022, 111: 109102. 4. Wang C, Chen R, Zhu X, et al.METTL14 alleviates the development of osteoporosis in ovariectomized mice by upregulating m6A level of SIRT1 mRNA.Bone.2022: 116652. 5. Huang L, Li Q. Notoginsenoside R1 promotes differentiation of human alveolar osteoblasts in inflammatory microenvironment through inhibiting NF‑κB pathway and activating Wnt/β‑catenin pathway. Molecular Medicine Reports. 2020, 22(6): 4754-4762 6. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker. British Journal of Pharmacology. 2021 Jul;178(13):2617-2631. doi: 10.1111/bph.15441. Epub 2021 May 20. 7. Zhang D, Li X, Hu Y, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination. Biochemical Pharmacology. 2018, 154: 183-192 8. Ding C, Fu S, Chen X, et al. Epigallocatechin gallate affects the proliferation of human alveolar osteoblasts and periodontal ligament cells, as well as promoting cell differentiation by regulating PI3K/Akt signaling pathway. Odontology. 2021 Jul;109(3):729-740. doi: 10.1007/s10266-021-00597-1. Epub 2021 Mar 6. 9. Chen Q Z, Li Y, Shao Y, et al. TGF-β1/PTEN/PI3K signaling plays a critical role in the anti-proliferation effect of tetrandrine in human colon cancer cells. International Journal of Oncology. 2017, 50(3): 1011-1021 10. Tian S, Wang R, Chen S, et al. Structural Basis for PPARs Activation by the Dual PPARα/γ Agonist Sanguinarine: A Unique Mode of Ligand Recognition. Molecules. 2021, 26(19): 6012.
Allicin Y13g dihydrochloride NDI-034858 Cephalandole B MyD88-IN-1 JC2-11 Dersalazine NO-prednisolone

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 药物功能重定位化合物库 口服活性化合物库 临床期小分子药物库 抗菌活性库 FDA 上市药物库 NMPA中国上市药物库 外泌体相关化合物库 临床前化合物库 人代谢物化合物库

剂量换算

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体内实验配液计算器

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。

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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。

Keywords

Dexamethasone 50-02-2 Autophagy Endocrinology/Hormones Immunology/Inflammation Microbiology/Virology IL Receptor Glucocorticoid Receptor Mitophagy Antibacterial SARS-CoV Complement System Antibiotic MK 125 receptor SARS coronavirus inhibit Hexadecadrol Prednisolone F Mitochondrial Autophagy CD18 CD62L glucocorticoid Inhibitor monocytes neutrophils Bacterial NSC 34521 地塞米松 CD11b inhibitor

 

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