Dexamethasone

产品编号: T1076 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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CAS：50-02-2

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生物活性化学信息储存和溶解度信息参考文献引用文献

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].

Cas No.

50-02-2

分子式

C22H29FO5

分子量

392.46

别名

MK 125;Hexadecadrol;Prednisolone F;NSC 34521;地塞米松;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]Zhang, Depeng, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination[J]. Biochemical pharmacology. 2018 Aug;154:183-192.[3]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.[4]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.[5]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.[6]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.[7]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.[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[J]. Odontology. 2021: 1-12.[9]Mulatero P, et al. Impaired cortisol binding to glucocorticoid receptors in hypertensive patients. Hypertension. 1997 Nov;30(5):1274-8.

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

剂量换算 Dexamethasone 50-02-2

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要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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Keywords

MK 125 receptor SARS coronavirus inhibit Mitophagy Hexadecadrol Prednisolone F Mitochondrial Autophagy CD18 CD62L Glucocorticoid Receptor glucocorticoid Inhibitor monocytes Antibiotic Dexamethasone neutrophils Bacterial Complement System NSC 34521 地塞米松 CD11b Autophagy SARS-CoV 50-02-2

Dexamethasone 相关推荐

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Dexamethasone

MK 125,Hexadecadrol,Prednisolone F,NSC 34521,地塞米松

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