1、Product Data SheetFenretinideCat. No.: HY-15373CAS No.: 65646-68-6分式: CHNO分量: 391.55作靶點: RAR/RXR; Autophagy作通路: Metabolic Enzyme/Protease; Autophagy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 : 130 mg/mL (332.01 mM)* means soluble, but saturation unknown.Solv

2、entMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.5540 mL 12.7698 mL 25.5395 mL5 mM 0.5108 mL 2.5540 mL 5.1079 mL10 mM 0.2554 mL 1.2770 mL 2.5540 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?shù)娜芙?/p>

3、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，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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: 2.5 mg/mL (6.38 mM); Clear solution此案可獲得 2.5 mg/mL (6.38 mM，飽和度未知) 的澄清溶液。以 1 mL

4、作液為例，取 100 L 25.0 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: 2.5 mg/mL (6.38 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (6.38 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DM

5、SO 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: 2.5 mg/mL (6.38 mM); Clear solution此案可獲得 2.5 mg/mL (6.38 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 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Fenretinide (4-HPR)種合成的類維素A衍物，能夠結(jié)合視黃酸受體

6、(RAR) 誘導(dǎo)細胞死亡。體外研究 Fenretinide (4-HPR) exerts not just acute but also long term antitumor activity in selected T-ALL cell lines. Fenretinideinhibits DES activity in CCRF-CEM leukemia cells in a dose and time dependent manner, leading to a concomitantincrease of the endogenous cellular dhCer content.

7、Fenretinide (3 M)-induced dhCer accumulation in both CCRF-CEM and Jurkat cells1. Ceramide inhibition with fenretinide protects insulin signaling. Fenretinide prevents lipid-induced reductions in insulin-stimulated glucose uptake2. Fenretinide inhibits OVCAR-5 cell proliferation andviability at conce

8、ntrations higher than 1 microM, with 70-90% growth inhibition at 10 microM. Fenretinide (1 microM)significantly inhibits OVCAR-5 invasion after 3 days preincubation. Endothelial cells treated with 1 microM 4-HPR failsto form tubes, but forms small cellular aggregates4.體內(nèi)研究 Fenretinide (4-HPR) (10 mg

9、/kg, i.p.) selectively inhibits ceramide accumulation HFD-fed male C57Bl/6 mice. Fenretinide treatment improves glucose tolerance and insulin sensitivity as determined by both glucose and insulin tolerance tests2. Addition of 25 mg/kg ketoconazole to Fenretinide in NOD/SCID mice increased 4-HPR plas

10、malevels3.PROTOCOLCell Assay 1 Standard XTT assay is used to determine cell viability. For fenretinide-only treatments, cells are plated in 96-wellplates at 750,000 cells/mL and 100 L/well. After 4 h, treatments are added on 50 L/well obtaining a final density of500,000 cells/mL and final volume of

11、150 L/well. Four replicates are used per experimental condition. XTT reagentmixture is added 4 h before the end of selected treatment period and absorbance at 490 nm is determined per eachwell. A slightly modified protocol is used for analysis of the effect of myriocin (final concentration of 100 nM

12、) orantioxidant on Fenretinide treatment. Briefly, cells are seeded on 60 mm culture dishes and myriocin or antioxidantsadded after 4 h. Fenretinide treatment is added 2 h later and cells are plated in quadruplicates in 96 well plates (150L/well).MCE has not independently confirmed the accuracy of t

13、hese methods. They are for reference only.Animal Male mice (C57Bl6) are fed a standard chow or a high-fat diet (HFD) from 5 to 17 weeks, at which point half of theAdministration 2 HFD-fed mice begin receiving fenretinide in drinking water for 4 weeks. Fenretinide is dissolved in 100% ethanol anddilu

14、ted in water to 10 g/mL. Control treatment water receives an equal amount of ethanol (0.5%). FEN water isprepared in low-light conditions and administered in light-protective bottles. Water is replaced every 1-2 days, andno precipitation of FEN is noted at any time. Animal weights are recorded at th

15、e beginning and end of the treatmentperiod. Following a 4-week FEN treatment, mice undergo intraperitoneal glucose and insulin tolerance tests. For bothtests, mice are fasted for 6 h andreceive an injection of either glucose (1 g/kg of body weight) or insulin (0.75units/kg of body weight). Blood glu

16、cose is determined at the times indicated by the Bayer Contour glucose meter,and insulin is measured with the rat/mouse insulin ELISA kit. The insulin resistance index is assessed by using fastingPage 2 of 3 www.MedChemEblood glucose and insulin levels to compute the homeostatic model assessment of

17、insulin resistance (HOMA-IR),where a higher number represents greater insulin resistance.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 Biomed Pharmacother. 2020 Feb 21;125:109680. J Cancer. 2019; 10(27):6767-6778. Oncol Rep. 2018 Jul;40(1)

18、:518-526. Cornea. 2018 Dec;37(12):1579-1585. Patent. 20200038327A1.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Apraiz, Aintzane., et al. Dihydroceramide accumulation and reactive oxygen species are distinct and nonessential events in 4-HPR-mediated leukemiacell death. Biochemistry and Cell Biology (2012), 90(2), 209-223.2. Bikman, Benjamin T., et al. Fenretinide Prevents Lipid-induced Insulin Resistance by Blocking Ceramide Biosynthesis. Journ