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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalidrosideCat. No.: HY-N0109CAS No.: 10338-51-9Synonyms: Rhodioloside分式: CHO分量: 300.3作靶點: mTOR作通路: PI3K/Akt/mTOR儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 H2O : 100 mg/m
2、L (333.00 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.3300 mL 16.6500 mL 33.3000 mL5 mM 0.6660 mL 3.3300 mL 6.6600 mL10 mM 0.3330 mL 1.6650 mL 3.3300 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。BIOLOGICAL ACTIVITY物活性 Salidroside種脯氨酰內(nèi)肽酶 (prolyl en
3、dopeptidase) 抑制劑。Salidroside 可通過激活 mTOR 信號緩解腫瘤惡病質(zhì)模型中的惡病質(zhì)癥狀。IC50 & Target mTOR體外研究Salidroside (100 M) inhibits prolyl endopeptidase (PEP) activity (10.61.9%). Prolyl endopeptidase is an1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEenzyme that plays a role in the metabolism of proline-containing ne
4、uropeptidase which is recognized to beinvolved in learning and memory 1. Salidroside, one of the major phenylpropanoid glycosides found in R.rosea L, is consumed almost daily as a nutritional supplement in many countries and has been identifiedpossessing potential anti-fatigue and anoxia,anti-aging,
5、 and anti-Alzheimers disease activities. Salidrosidecan improve muscle nutrition via increasing mTOR, p-mTOR, and MyHC expression 2. SH-SY5Y cells areexposed to 0-600M MPP+ for 12-48h and the results show that MPP+ results in a significant decrease ofcell viability in a concentration and time-depend
6、ent manner. Cells are pretreated with 25-100M Salidroside(Sal) for 24h and then exposed to 500M MPP+ for an additional 24h. Salidroside concentration-dependently prevents MPP+-induced decrease of cell viability. Annexin V/PI staining is a common method forthe detection of apoptotic cell. Salidroside
7、 significantly decreases the number of Annexin V/PI-stained cellstreated by MPP+ which is in a concentration-dependent manner. Apoptotic cell could also be morphologicallyevaluated by Hoechst staining. In Hoechst staining, apoptotic cells are characterized by reduced nuclearsize, chromatin condensat
8、ion, intense fluorescence, and nuclear fragmentation. Salidroside notably inhibitsMPP+-induced increase of chromatin condensation, intense fluorescence, and nuclear fragmentation in SH-SY5Y cells 3.體內(nèi)研究 Salidroside is a natural antioxidant extracted from medicinal food plant Rhodiola rosea. Salidros
9、ide (100mg/kg/day) shows strong glucose lowering effect on db/db mice which is similar to effect of Metformin (200mg/kg/day). For this reason, the dose of 100 mg/kg/day salidroside is used 4.PROTOCOLCell Assay 3 SH-SY5Y cells are seeded in 96-well plates at 1104 cells per well. After the treatment w
10、ith Salidroside (25-100M) and MPP+, cell viability is measured by MTT assay. Briefly, cells are incubated with 500g/mL MTTat 37C for 4h. After that, the medium is removed and 150L DMSO is added and shaking is conducted for10min. Absorbance is measured at 570nm in a microplate reader and the results
11、are expressed as folds ofcontrol 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 4Administration 4 The 4-week-old male C57BL/6 mice are fed a high-fat diet (HFD) (n=16) or normal chow diet (n=8). After 10weeks of the HFD, salidroside inter
12、vention (100 mg/kg/day) is initiated by gavage once a day for 5 weeks.The control groups are given vehicle (saline). The 4-week-old male C57Bl/KsJ (BKS) mice (wild type, n=8)and BKS.Cg-Dock7m +/+ Leprdb/J (db/db) mice (n=16) are used. Salidroside (100 mg/kg/day) isadministrated orally by gavage once
13、 a day for 5 weeks. The control groups are given vehicle (saline). Fastingblood glucose and body weight of mice are monitored every 5 days. Glucose measurements are performedon blood drawn from the tail vein using a Glucometer.MCE has not independently confirmed the accuracy of these methods. They a
14、re for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Invest Ophthalmol Vis Sci. 2019 May 1;60(6):2072-2082.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Int J Oncol. 2019 Apr.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Fan W, et al. Prolyl endopeptidase inhibitors from the underground par
15、t of Rhodiola sachalinensis. Chem Pharm Bull (Tokyo). 2001Apr;49(4):396-401.2. Chen X, et al. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activatingmTOR signalling. J CachexiaSarcopenia Muscle. 2016 May;7(2):225-32.3. Wu L, et al. Salidroside Protects against MPP+-Induced Neuronal Injury through DJ-1-Nrf2 Antioxidant Pathway. Evid BasedComplement Alternat Med. 2017;2017:5398542.4. Ju L, et al. Salidroside, A Natural Antioxidant, Improves -Cell Survival and Function via Activating AMPK Pathwa
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