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TargetMol.T1076 .Dexamethasone地塞米松
  • 品牌:TargetMol
  • 型号:1 g
  • 货号:T1076
  • cas:50-02-2
  • 价格: ¥760/瓶
  • 发布日期: 2023-05-08
  • 更新日期: 2024-08-30
产品详请
产地
品牌 TargetMol
货号 T1076
用途
英文名称
包装规格 1 g
纯度 %
CAS编号 50-02-2
别名 地塞米松
分子式
是否进口
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].
Cas No.
50-02-2
分子式
C22H29FO5
分子量
392.46
别名
地塞米松;Hexadecadrol;MK 125;NSC 34521;Prednisolone F;Dexamethasone
参考文献
[1]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 [2]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. [3]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. [4]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. [5]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. [6]Zhang, Depeng, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination[J]. Biochemical pharmacology. 2018 Aug;154:183-192. [7]Mulatero P, et al. Impaired cortisol binding to glucocorticoid receptors in hypertensive patients. Hypertension. 1997 Nov;30(5):1274-8. [8]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. [9]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.
引用文献
[1]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. [2]Sun C, Li X, Guo E, et al. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis. Oncogene. 2019: 1-15. [3]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 [4]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 [5]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. [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. Molecular Medicine Reports. 2020, 22(6): 4754-4762 [7]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.
储存和溶解度
Ethanol:6 mg/mL (15.28 mM)
DMSO:73 mg/mL (186 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years