磷酸奧司他韋作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetOseltamivir phosphateCat. No.: HY-17016CAS No.: 204255-11-8分式: CHNOP分量: 410.4作靶點(diǎn): Influenza Virus作通路: Anti-infection儲(chǔ)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(shí)驗(yàn) H2O : 100 mg/mL (243.66 mM; Need ultrasonic)DMSO : 100 mg/mL (243.66 mM; Need ultrason

2、ic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.4366 mL 12.1832 mL 24.3665 mL5 mM 0.4873 mL 2.4366 mL 4.8733 mL10 mM 0.2437 mL 1.2183 mL 2.4366 mL請(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式

3、選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.09 mM); Clear solution此案可獲得 2.5 mg/mL (6.09 mM，飽和度未知) 的澄清溶液。

4、以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.09 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (6.09 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/m

5、L 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。BIOLOGICAL ACTIVITY物活性 Oseltamivir phosphate (GS 4104)。種神經(jīng)氨酸酶 (neuraminidase) 抑制劑，于預(yù)防和治療流感 (influenza A 和 B)IC & Target Influenza A and B1體外研究 Oseltamivir phosphate (OP) is a prodrug that is readily absorbed from the gastrointestinal tract after oraladmi

6、nistration and is extensively converted predominantly by hepatic esterases to Oseltamivir carboxylate (OC)1.Oseltamivir phosphate is a widely used anti-influenza sialidase inhibitor. The metabolic activity of CMA07 and CMT-U27 cell lines is significantly decreased with 305 M Oseltamivir phosphate tr

7、eatment (p=0.005 and p0.0001respectively) using One Way ANOVA testes. In contrast, no statistically significant alterations are observed with 0.305M (p=0.9781), 3.05 M (p=0.7436) and 30.5 M (p=0.9623) of Oseltamivir phosphate treatments when comparewith control cells. Finally, to assess the effect o

8、f Oseltamivir phosphate on CMA07 and CMT-U27 programmed celldeath, and given that 305 M Oseltamivir phosphate treatment impaired cell metabolic activity, a programmed celldeath measurement is performed with the TUNEL assay. Twenty-four hour Oseltamivir phosphate treatment,specifically at 305 M, sign

9、ificantly increases CMA07 (p=0.001) and CMT-U27 (p=0.0002) DNA fragmentation,suggesting promotion of programmed cell death, when compare with lower Oseltamivir concentrations, or with PBS2.體內(nèi)研究 Oseltamivir phosphate-treated mice present significantly more inflammatory infiltrate in primary tumors (p

10、=0.01). Ki-67 antigen and caspase-3 protein are used to assess CMT-U27 xenograft tumor cell proliferation and apoptosis respectively. Virtually no differences are found in Ki-67 and caspase 3 (p=0.2) expression between Oseltamivir-treatedand non-treated mice2.PROTOCOLCell Assay 2 CMA07 and CMT-U27 c

11、ells are cultured in 24-well plates in triplicate for each condition: 0.305 M, 3.05 M, 30.5 Mand 305 M Oseltamivir phosphate and PBS is used as control. Cells are counted every day for 7 days in a Neubauerschamber in a 1:2 dilution of cells in 0.4% trypan blue and cell count is done using the volume

12、 conversion factor for 1mm3, which is 1104. This assay is repeated 3 times and growth curves are traced2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice2Administration 2 Female NIH(S)II-nu/nu nude mice, aged 4-6 weeks, are orthotopically ino

13、culated with 1106 viable CMT-U27 caninebreast cancer cells in the mammary fat pad using a 25 gauge needle. A total of 8 mice are inoculated. When nodulesreached a volume of approximately 500 mm3, mice (n=8) are randomized and divided into control group (n=4) andtreatment group (n=4).The animals rece

14、ive intraperitoneally (IP) dailly either 100 L of PBS (control group) or100mg/Kg of Oseltamivir phosphate, diluted in PBS (treatment group) until time of death. Tumor size is measuredusing calipers, and tumor volume (mm3) is estimated by widthlengthheight.MCE has not independently confirmed the accu

15、racy of these methods. They are for reference only.Page 2 of 3 www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Chemosphere. 2015 Jul;131:41-7. Int J Mol Sci. 2019 Dec 12;20(24). pii: E6261. Antiviral Res. 2020 Feb 20:104751. Biomed Pharmacother. 2018 Jan;97:385-394. Virology. 2020 Feb.See more customer validations on HYPER

16、LINK www.MedChemE www.MedChemEREFERENCES1. Huang H, et al. Transplacental transfer of Oseltamivir phosphate and its metabolite Oseltamivir carboxylate using the ex vivo human placenta perfusionmodel in Chinese Hans population. J Matern Fetal Neonatal Med. 2016 Aug 8:1-5.2. de Oliveira JT, et al. Anti-influenza neuraminidase inhibitor Oseltamivir phosphate induces canine mammary cancer cell aggressiveness. PLoS One. 2015Apr 7;10(4):e0121590.3. Li P, et al. A Simple and Robust Approach for Evaluation of Antivirals Using a Recombinant Influenza Virus Expressing Gaussia Luciferase. Vir