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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMelatoninCat. No.: HY-B0075CAS No.: 73-31-4Synonyms: N-Acetyl-5-methoxytryptamine分式: CHNO分量: 232.28作靶點: Melatonin Receptor; Autophagy; Mitophagy; EndogenousMetabolite作通路: GPCR/G Protein; Neuronal Signaling; Autophagy; MetabolicE
2、nzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 68 mg/mL (292.75 mM)Ethanol : 50 mg/mL (215.26 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.3051 mL 21.5257 mL 43.0515 mL5 mM 0.8610 mL 4.3051 mL 8.
3、6103 mL10 mM 0.4305 mL 2.1526 mL 4.3051 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)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?,再依次添加助溶?為保證實驗結(jié)果的可靠性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當(dāng)天使;澄清的儲備液可以根據(jù)儲存條件,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% EtOH 40% PEG300 5% Tween-80 45% saline1/3 Master of Small Molecules 您
4、邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (10.76 mM); Clear solution2. 請依序添加每種溶劑: 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.76 mM); Clear solution3. 請依序添加每種溶劑: 10% EtOH 90% corn oilSolubility: 2.5 mg/mL (10.76 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Melatonin種由松果體制成的激素,可激活褪激素受體。 M
5、elatonin在睡眠中起作并具有重要的抗氧化和抗炎特性。IC50 & Target Human Endogenous Metabolite體內(nèi)研究 Melatonin increases the levels of activated PTEN, RSK-1, mTOR and AMPK kinases, mildly inhibits ERK-1/2 phosphorylation and Bad phosphorylation, significantly inhibits phosphorylations of S6 RibosomalProtein, 4E-BP1, GSK-3 an
6、d GSK-3, and slightly increases PRAS40 phosphorylation in animals 1.Melatonin ameliorates the neurotoxiciy and astrocyte activation induced by A1-42 in the cerebral cortex.Melatonin also blocks the reduction in Reelin and Dab1 expression induced by A1-42 2. Melatonintreatment and lack of NLRP3-/- sh
7、are similar inhibition of NF-B and NLRP3 signaling pathway in mice.Melatonin treatment and lack of NLRP3-/- share some patterns of clock genes expression, and improvecardiomyocytes morphology in mice 3.PROTOCOLAnimal A total of two sets of adult male C57BL/6j mice weighing 21-26 g are randomly assig
8、ned to one of fourAdministration 1 groups and treated with intraperitoneal (i.p.) delivery of (i) vehicle (50 L isotonic saline/5% ethanol), (ii)melatonin (4 mg/kg, dissolved in 0.9% isotonic saline/5% ethanol), (iii) Wortmannin, and (iv)melatonin/Wortmannin immediately after reperfusion. In the fir
9、st set, mice are exposed to 30 min of focalcerebral ischemia (FCI) and 72 h reperfusion for the evaluation of disseminate ischemic injury in the striatum,and signaling pathway analysis (n=7 per group). The second group of mice is exposed to 90 min of FCI and24 h reperfusion for the analysis of infar
10、ct development, brain swelling and IgG extravasation (n=7 pergroup).MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Redox Biol. 2019 May 20;24:101225 J Cell Mol Med. 2018 Oct;22(10):5132-5144. Molecules. 2018 Mar 16;23(3). pii: E675.See more
11、 customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEREFERENCES1. Kilic U, et al. Particular phosphorylation of PI3K/Akt on Thr308 via PDK-1 and PTEN mediates melatonins neuroprotective activity afterfocal cerebral ischemia in mice. Redox Biol. 2017 Apr 5
12、;12:657-6652. Hu C, et al. Neuroprotective effect of melatonin on soluble A1-42-induced cortical neurodegeneration via Reelin-Dab1 signalingpathway. Neurol Res. 2017 Apr 7:1-13. Rahim I, et al. Melatonin administration to wild-type mice and non-treated NLRP3 mutant mice share similar inhibition of theinflammatory response during sepsis. J Pineal Res. 2017 Mar 31McePdfHeightCaution
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