莫能菌素鈉鹽作用機制 - Medchemexpress - MCE中國

1、Product Data SheetMonensin sodium saltCat. No.: HY-N0150CAS No.: 22373-78-0分式: CHNaO分量: 692.85作靶點: Bacterial; Sodium Channel作通路: Anti-infection; Membrane Transporter/Ion Channel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 Ethanol : 25 mg/mL (36.08 mM; Need ultrason

2、ic)DMSO : 1 mg/mL (insoluble or slightly soluble)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.4433 mL 7.2166 mL 14.4331 mL5 mM 0.2887 mL 1.4433 mL 2.8866 mL10 mM 0.1443 mL 0.7217 mL 1.4433 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 mon

3、ths; -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)娜芙獍?。以下溶解案都請先按?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% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/m

4、L (3.61 mM); Suspended solution; Need ultrasonic此案可獲得 2.5 mg/mL (3.61 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。2. 請依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 2.5 mg/mL (3.61 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (3.61 mM，飽

5、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 25.0 mg/mL 的澄 EtOH 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Monensin sodium salt 由桂鏈霉 介導(dǎo) Na+/H+ 交換的離載體。(Streptomyces cinnamonensis) 分泌的抗素。Monensin sodium salt 種IC & Target bacterial1體外研究 Monensin sodium salt is an antibiotic secreted by the bacter

6、ia Streptomyces cinnamonensis. Untreated cells display2.5% apoptosis; 48 hours treatment with 1 M Monensin sodium salt shows 4.5% apoptosis whereas 5 M Monensinsodium salt for 48 hours induces a greater apoptotic response (16.4%). Pretreatment with either 1 or 5 M Monensinsodium salt for 24 hours fo

7、llowed by 10 M erlotinib treatment for another 24 hours results in a marked increases inapoptotic events (14.6% and 38.7%, respectively) when compare with either Monensin sodium salt or erlotinibtreatments alone. Combination of 5 M Monensin sodium salt with 10 M erlotinib shows the highest percentag

8、e ofapoptosis (38.7%)1.體內(nèi)研究 Although the numbers of tumors do not change substantially, a significant (P=0.0144) reduction in the average size oflesions is observed in Monensin sodium salt-treated Apc+/Min mice when compare with control animals (mean 0.199mm2 vs. 0.299 mm2). The total tumor area est

9、imated in one animal is decreased in individuals receiving Monensinsodium salt (mean 10.16 mm2 vs. 16.46 mm2; P=0.0125). Monensin sodium salt treatment increases the numbers ofapoptotic cells and cells expressing the p21 cell-cycle inhibitor at the surface area of the neoplastic outgrowths. Nochange

10、s in the cell proliferation, differentiation, and tissue architecture in the healthy parts of mucosa are noted afterexposure to Monensin sodium salt2.PROTOCOLCell Assay 1 One million SCC25 cells are seeded in 10-cm plates and incubated overnight to allow for attachment and recovery.The following day

11、, cells are pretreated with 0, 1, or 5 M Monensin sodium salt for 24 hours then treated with 10 M erlotinib alone or in combination with Monensin sodium salt for a further 24 hours. Adherent and cells insuspension are collected by centrifugation and fixed in 3 mL of cold 80% ethanol overnight at -20

12、C. Before analysis,cell pellets are washed with PBS resuspended in staining buffer containing 25 g/mL propidium iodide and 40 g/mLRNase A and incubated for a minimum of 1 hour in the dark at room temperature1.MCE has not independently confirmed the accuracy of these methods. They are for reference o

13、nly.Animal Multiple intestinal neoplasia (Min) mice are used in this study. Four-week-old pups are weaned, genotyped, andAdministration 2 randomized. The animals are divided into two groups and treated with Monensin sodium salt (10 mg/kg) or vehicle(DMSO). Daily oral applications continue for 6 week

14、s. In addition, six pairs of Apc+/Min mice age 7, 10, 13, 16, 19, and22 weeks are treated with Monensin sodium salt or vehicle for 5 weeks. The mice are sacrificed and the intestines aredissected, washed in PBS, and fixed in 4% formaldehyde (v/v) in PBS for 3 days. Fixed intestines are embedded inpa

15、raffin, sectioned and stained. The number and size of the neoplastic lesions are quantified using Ellipse software2.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Page 2 of 3 www.MedChemE Front Microbiol, 30 April 2020See more customer valid

16、ations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Dayekh K, et al. Monensin inhibits epidermal growth factor receptor trafficking and activation: synergistic cytotoxicity in combination with EGFRinhibitors. Mol Cancer Ther. 2014 Nov;13(11):2559-71.2. Tumova L, et al. Monensin inhibits canonical Wnt signaling in human colorectal cancer cells and suppresses tumor growth in multiple intestinal neoplasiamice. Mol Cancer Ther. 2014 Apr;13(4):812-22.3. Youhua Huang, et al. Autophagy Participates in Lysosomal Vacuolation-Mediated Cell Death in RGNNV-Infected Cells.