厄多司坦作用機制 - Medchemexpress - MCE中國

1、Product Data SheetErdosteineCat. No.: HY-B0289CAS No.: 84611-23-4分式: CHNOS分量: 249.31作靶點: NF-B; Bacterial作通路: NF-B; Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (200.55 mM; Need ultrasonic)H2O : 6.67 mg/mL (26.75 mM; Need ultrasonic)Sol

2、ventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 4.0111 mL 20.0554 mL 40.1107 mL5 mM 0.8022 mL 4.0111 mL 8.0221 mL10 mM 0.4011 mL 2.0055 mL 4.0111 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜?/p>

3、解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3.25 mg/mL (13.04 mM); Clear solution此案可獲得 3.25 mg/mL (13.04 mM，飽和度未知) 的澄清溶液。以

4、1 mL 作液為例，取 100 L 32.5 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.25 mg/mL (13.04 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 3.25 mg/mL (13.04 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 32.5 mg

5、/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3.25 mg/mL (13.04 mM); Clear solution此案可獲得 3.25 mg/mL (13.04 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 32.5 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Erdosteine 抑制脂多糖 (LPS) 誘導(dǎo)的

6、NF-B 激活。Erdosteine 具有粘液調(diào)節(jié)，抗，抗炎和抗氧化作。IC & Target NF-B體外研究 Erdosteine is an oral mucolytic agent used as an expectorant in various chronic respiratory diseases. Erdosteine exertsanti-inflammatory effects by inhibiting NF-B activation in LPS-stimulated mouse macrophages. However, Erdosteinedoes not inh

7、ibit LPS induced phosphorylation of the Akt and MAPK pathways. To evaluate the toxic effects ofErdosteine on macrophages, cell viability is analyzed. Treatment with 1, 10, or 100 g/mL Erdosteine does notproduce detectable cytotoxicity. Treatment with LPS (1 g/mL) induced IB degradation in RAW 264.7

8、cells, andmaximal degradation is observed after 10 min. RAW 264.7 cells are pretreated with the indicated concentrations ofErdosteine for 6 h and then stimulated with LPS (1 g/mL) for 10 min. Pretreatment with Erdosteine does not haveany effect on the baseline amount of IB. Treatment with DMSO alone

9、 at a volume equal to that used for Erdosteinedelivery does not have any effect on the baseline amount of IB. The amount of IB is decreased by treatment withLPS for 10 min, and pretreatment with Erdosteine at the indicated concentration and time effectively inhibits IBdegradation1.體內(nèi)研究 Twenty-six ma

10、le mice are divided into four groups as follows: group 1, control; group 2, Erdosteine-treated; group 3,Methotrexate (MTX)-treated; and group 4, Methotrexate+Erdosteine treated. On the first day of experiment, a singledose of Methotrexate is intraperitoneally administered to groups 3 and 4, although

11、 a daily single dose of Erdosteineis orally administered to group 2 and 4 for 7 days. At the end of the experiment, the testes of the animals areremoved and weighed. The levels of total antioxidant capacity and total oxidative stress, and myeloperoxidase activityin the Methotrexate group are higher

12、than the control group (p0.05). Lipid peroxidation levels are not changed inMethotrexate group compared with control group. In conclusion, Erdosteine can effectively protect the testes inMethotrexate-induced toxicity. Erdosteine administration with Methotrexate improves testicular injures, as indica

13、tedby appearance of spermatogenesis in seminiferous tubules2.PROTOCOLCell Assay 1 The murine macrophage/monocyte cell line RAW264.7 are maintained as monolayers in Dulbeccos modified Eaglesmedium (DMEM) containing 10 % fetal bovine serum, 60 U/mL Penicillin, and 100 g/mL Streptomycin at 37.8C in 5%

14、CO2. The cell viability is quantified using a colorimetric tetrazolium compound MTS assay. Briefly, 1104 cellsincubated with various concentrations of Erdosteine (1, 10, or 100 g/mL) for 24 h are treated with 10 L of MTSsolution (5 mg/mL) for 45 min. The cells are then lysed with isopropyl alcohol,

15、and the absorbance is read at thewavelength of 540 nm1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Page 2 of 3 www.MedChemEAdministration 2 Twenty-six male C57BL/6 mice (8 weeks, 20-30 g) are randomly divided into four groups. In control

16、 group (n=6);mice are treated the 0.5 mL of saline as a placebo intraperitoneally (i.p.). In Erdosteine group (n=6), mice are treatedwith Erdosteine orally (gavage; 10 mg/kg) for 7 days. In this study, low-dose MTX are used because high-dose (20-40 mg/kg) MTX has anti-inflammatory and immunosuppress

17、ive activity. Mice in MTX group (n=7) are injected withsingle dose of i.p. MTX (10 mg/kg). In MTX+Erdosteine group (n=7), mice are injected with single dose of i.p. MTX (10mg/kg) the first day and Erdosteine is given orally (10 mg/kg) to the animals starting the first day for 7 days. After thelast a

18、dministration of the drug, all rats fasted about 12 hours, but have free access to water. And then, the animalsare sacrificed by cervical dislocation at the end of the experiment. Following sacrifice, the testes are quickly removedfrom the mice. Right testes specimens are fixed in 10% neutral-buffered formaldehyde solution for histologicalassessment2.MCE has not independently confirmed the accuracy of these methods. They are for referen