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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPolyoxyethylene stearateCat. No.: HY-101530CAS No.: 9004-99-3Synonyms: POES分式: CHO分量: 328.53作靶点: P-glycoprotein作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验
2、DMSO : 49 mg/mL (149.15 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0439 mL 15.2193 mL 30.4386 mL5 mM 0.6088 mL 3.0439 mL 6.0877 mL10 mM 0.3044 mL 1.5219 mL 3.0439 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Polyoxyethylene
3、 stearate (POES)离乳化剂。体外研究Polyoxyethylene stearate has been recommended as an additive to the radiolabelled 7H12 Middlebrook TBmedia and as such has been shown to enhance growth of mycobacteria in the radiometric BACTEC rapidculture system. Polyoxyethylene (50) stearate produces the greatest enhancem
4、ent in growth and reduction in1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEthe time taken to detect growth for M. tuberculosis and polyoxyethylene (30) stearate and polyoxyethylene(JL) stearate for species of mycobacteria other than M. tuberculosis 1. Polyoxyethylene stearate inhibits P-gp media
5、ted efflux in a concentration dependent manner mainly by modulating substrate-stimulated P-gpATPase activity 2. Polyoxyethylene 40 stearate reduces vinblastine sulfate efllux. The cytotoxicity ofvinblastine to K562/ADR cells is significantly enhanced when the cells are cotreated with 100 or 150 g/mL
6、polyoxyethylene 40 stearate 3.体内研究 Polyoxyethylene stearate is potentially useful as a pharmaceutical ingredient to improve the oralbioavailability of coadministered P-gp substrates and substrates for certain CYP isoforms 2. The averagetumor volume and average tumor weight are significantly less in
7、the polyoxyethylene 40 stearate+vinblastinegroup. The inhibition rate for tumor growth is increased from 0.06 (vinblastine group) to 0.84(vinblastine+polyoxyethylene 40 stearate group) 3.PROTOCOLCell Assay 3 Polyoxyethylene 40 stearate is added to the test vinblastine solution. The cytotoxicity of v
8、inblastine toK562/ADR cells is then assessed. The final concentrations of polyoxyethylene 40 stearate are 0, 50, 100,and 150 g/mL. After 8 hours of treatment, cells are incubated for 4 hours in the presence of MTT reagentand then lysed with DMSO. Absorbance is measured at 490 nM 3.MCE has not indepe
9、ndently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Polyoxyethylene 40 stearate and vinblastine are dissolved in 0.9% sodium chloride solution, yielding aAdministration 3 solution of 200 g/mL VBL and 150 g/mL PS40. The drug is injected subcutaneously in a volume
10、 of 0.1 mLper 10 g of body weight at a dosage of 2 mg/kg vinblastine and 1.5 mg/kg polyoxyethylene 40 stearatearound the tumor every other day for 8 days. The volume of tumors and the weight of mice are measuredevery day from the day the tumors are formed 3.MCE has not independently confirmed the ac
11、curacy of these methods. They are for reference only.REFERENCES1. Cutler RR, et al. The effect of polyoxyethylene stearate (POES) on the growth of mycobacteria in radiometric 7H12 Middlebrook TBmedium. Tubercle. 1987 Sep;68(3):209-20.2. Zhu S, et al. Effects of polyoxyethylene (40) stearate on the activity of P-glycoprotein and cytochrome P450. Eur J Pharm Sci. 2009 Jul12;37(5):573-80.3. Luo L, et al. Polyoxyethylene 40 stearate modulates multidrug resistance and enhances antitumor activity of vinblastine sulfate. AAPS J.2007 Oct 5;9(3):E329-35.McePdfHeightCaution: Pro
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