地塞米松作用机制 - Medchemexpress - MCE中国

1、Product Data SheetDexamethasoneCat. No.: HY-14648CAS No.: 50-02-2分式: CHFO分量: 392.46作靶点: Glucocorticoid Receptor; Autophagy; Mitophagy; Complement System; Bacterial作通路: GPCR/G Protein; Autophagy; Immunology/Inflammation; Anti-infection储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1

2、month (protect from light)溶解性数据体外实验 DMSO : 56 mg/mL (142.69 mM)Ethanol : 8.33 mg/mL (21.23 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.5480 mL 12.7402 mL 25.4803 mL5 mM 0.5096 mL 2.5480 mL 5.0961 mL10 mM 0.

3、2548 mL 1.2740 mL 2.5480 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂

4、前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.37 mM); Clear solution此案可获得 2.5 mg/mL (6.37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理

5、盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.37 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (6.37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (

6、6.37 mM); Clear solution此案可获得 2.5 mg/mL (6.37 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Dexamethasone (Hexadecadrol)种糖质激素受体 (glucocorticoid receptor) 激动剂。Dexamethasone 还显着 降低中性粒细胞的 CD11b，CD18 和 CD62L 表达，以及单核细胞的 CD11b 和 CD18L

7、表达。IC & Target Glucocorticoid receptor1体外研究 Dexamethasone (Hexadecadrol) regulates several transcription factors, including activator protein-1, nuclear factor-AT, and nuclear factor-kB, leading to the activation and repression of key genes involved in the inflammatoryresponse1.Dexamethasone potentl

8、y inhibits granulocyte-macrophage colony stimulating factor (GM-CSF) release from A549cells with EC50 of 2.2 nM. Dexamethasone (EC50=36 nM) induces transcription of the 2-receptor is found to correlatewith glucocorticoid receptor (GR) DNA binding and occurred at 10-100 fold higher concentrations tha

9、n the inhibitionof GM-CSF release. Dexamethasone (IC50=0.5 nM) inhibits a 3B (NF-B, IB, and I-B), which is associated withinhibition of GM-CSF release2.体内研究 It has previously been reported that treatment with Dexamethasone (Hexadecadrol) at a dose of 25 mg/kg efficiently inhibits lipopolysaccharide

10、(LPS)-induced inflammation. In our experimental system, treatment with a single dose of Dexamethasone 10 mg/kg (i.p.) significantly decreases recruitment of granulocytes as well as spontaneousproduction of oxygen radicals compared with animals expose to LPS and injected with solvent alone (saline).

11、Theeffects are statistically significant when administered both 1 h before and 1 h after inhalation of LPS. The number ofgranulocytes in BALF decreased to levels comparable to healthy animals (given an aerosol of water)3.Rats treated with Dexamethasone consume less food and weighed less than control

12、 rats. Treated rats also weigh lessthan pair-fed animals though their food intake is similar. Five days of Dexamethasone injection result in a significantincrease in both the liver mass (+42%) and the liver to body weight ratio (+65%). The wet weight of gastrocnemiusmuscle decreases 20% after 5 days

13、 of treatment, but it remains unaffected relative to body weight (g/100 g bodyweight), indicating that muscle weight loss paralleled body weight loss4.PROTOCOLAnimal Mice3Administration 34 Female C57Bl/6JBom mice (age 10-12 weeks) are used in all experiments. Dexamethasone is administered as a singl

14、einjection of 1 or 10 mg/kg. Dexamethasone is dissolved in saline and 400 L are injected intraperitoneally, either 1 hbefore or 1 h after LPS exposure. In one experiment, N-acetylcysteine (NAC) (100 and 500 mg/kg) is injectedsuccessively every 45 h, starting 1 h before challenge (five injections in

15、total). A control group of LPS-exposedanimals are injected intraperitoneally with solvent alone (saline). Intratracheal administration is performed byinstillation of 100 L NAC (50, 100 or 500 mg/kg) or Dexamethasone (10 mg/kg) into the lungs of mice.Rats4Male Sprague-Dawley rats are used.Dexamethaso

16、ne-treated rats are injected intraperitoneally once daily withPage 2 of 3 www.MedChemEDexamethasone (1.5 mg/kg body weight) for 5 days and are allowed to feed ad libitum. The Dexamethasone dose(1.5 mg/kg/day) and the duration of treatment (5 days) are specifically chosen as this treatment induced ar

17、eproducible and marked catabolic state. Control rats received no treatment and are fed ad libitum. In order to takeinto account the decrease in food intake induced by Dexamethasone treatment, a third group of pair-fed rats areused. These rats are provided with the same amount of food as Dexamethason

18、e-injected rats and are treated with adaily isovolumic intraperitoneal injection of NaCl (0.9%) for 5 days. After the final injection of Dexamethasone orNaCl, the animals are fasted overnight prior to being killed by decapitation.MCE has not independently confirmed the accuracy of these methods. The

19、y are for reference only.户使本产品发表的科研献 Biomaterials. 2020 Feb;232:119730. Chem Mater. 2017, 29(19):8221-8238. J Med Chem. 2019 Jul 25;62(14):6561-6574. Acta Pharmacol Sin. 2020 May 12. Toxicol Lett. 2019 Jul;309:42-50.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. LaL

20、one CA, et al. Effects of a glucocorticoid receptor agonist, Dexamethasone, on fathead minnow reproduction, growth, and development. EnvironToxicol Chem. 2012 Mar;31(3):611-22.2. 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):1003-113. Rocksn D, et al. Differential anti-inflammatory and anti-oxidative effects of Dex