Edaravone-MCI-186-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEdaravoneCat. No.: HY-B0099CAS No.: 89-25-8Synonyms: MCI-186分式: CHNO分量: 174.2作靶點(diǎn): MMP作通路: Metabolic Enzyme/Protease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(shí)驗(yàn) DMSO : 125 mg/mL (717.57 mM; Need

2、 ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 5.7405 mL 28.7026 mL 57.4053 mL5 mM 1.1481 mL 5.7405 mL 11.4811 mL10 mM 0.5741 mL 2.8703 mL 5.7405 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，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥蔚膬湟海僖来翁砑又軇?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件

3、，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (11.94 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (11.94 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules

4、您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (11.94 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Edaravone種新穎的，有效的由 MMP-9 有關(guān)的腦出。體外研究 Edaravone performs both preventative and therapeutic effects against toxicity of glutamate. Pretreatment ofedaravone reduces the toxicity of glutamate towards SGNs. Edaravon

5、e reduces apoptosis and necrosiscaused by glutamate. Pretreatment of edaravone (500M) reverses these changes to approximately normallevels. The protective effect of edaravone on SGNs against glutamate-induced apoptosis is associated withPI3K/Akt pathway and Bcl-2 protein family 4.體內(nèi)研究 Edaravone exer

6、ts neuroprotective effects by inhibiting endothelial injury and by ameliorating neuronaldamage in brain ischemia. Edaravone provides the desirable features of NOS: it increases eNOS (beneficialNOS for rescuing ischemic stroke) and decreases nNOS and iNOS (detrimental NOS). Post-reperfusionbrain edem

7、a and hemorrhagic events induced by thrombolytic therapy may be reduced by edaravonepretreatment 1. Edaravone significantly decreases infarct volume, with the average infarct volume in theedaravone-treated rats (227.6 mm3) being significantly lower than that in the control rats (264.0 mm3).Edaravone

8、 treatment also decreases the postischemic hemorrhage volumes (53.4 mm3 in edaravone-treatedrats vs 176.4 mm3 in controls). In addition, the ratio of hemorrhage volume to infarct volume is lower in theedaravone-treated rats (23.5%) than in the untreated rats (63.2%) 2. In edaravone (20 mg/kg)-treate

9、d rats,astrocyte activity (glial fibrillary acidic protein) and apoptotic cells (caspase-3) are decreased on the corpuscallosum, germinal matrix, and cerebral cortex 3.PROTOCOLCell Assay 4 Cell viability is quantified by MTT assay and trypan blue staining. MTT (5mg/mL, 20L) is added to each welland

10、incubated for 4h at 37C after the drug treatments. The medium is removed and the cell pellet isdissolved in DMSO. Then, the optical density (OD) values are measured at 570nm using an ELISA reader.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Planta M

11、ed. 2017 Feb;83(3-04):341-350.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Yoshida, H., et al. Neuroprotective effects of edaravone: a novel free radical scavenger in cerebrovascular injury. CNS Drug Rev, 2006.12(1): p. 9-20.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2

12、. Okamura, K., et al. Edaravone, a free radical scavenger, attenuates cerebral infarction and hemorrhagic infarction in rats withhyperglycemia. Neurol Res, 2013.3. Garcia CA, et al. Edaravone reduces astrogliosis and apoptosis in young rats with kaolin-induced hydrocephalus. Childs Nerv Syst. 2016Dec 17. Epub ahead of print4. Bai X, et al. Protective Effect of Edaravone on Glutamate-Induced Neurotoxicity in Spiral Ganglion Neurons. Neural Plast.2016;2016:4034218. Epub 2016 Nov 10.McePdfHeightC