Dexamethasone
產(chǎn)品名稱：Dexamethasone
產(chǎn)品描述：
| 產(chǎn)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 |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 動(dòng)物實(shí)驗(yàn) | 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]. |
| 別名 | MK 125, Hexadecadrol, Prednisolone F, NSC 34521, 地塞米松 |
| 化合物與蛋白結(jié)合的復(fù)合物 |
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 |
存儲(chǔ)
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 )
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