甲磺酸奈非那韋作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetNelfinavir MesylateCat. No.: HY-15287ACAS No.: 159989-65-8分式: CHNOS分量: 663.89作靶點(diǎn): HIV Protease; HIV作通路: Anti-infection; Metabolic Enzyme/Protease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) DMSO : 25 mg/mL (37.66 mM)* means soluble, but saturation

2、 unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 1.5063 mL 7.5314 mL 15.0627 mL5 mM 0.3013 mL 1.5063 mL 3.0125 mL10 mM 0.1506 mL 0.7531 mL 1.5063 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)

3、物和給藥式選擇適當(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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.77 mM); Clear solution此案可獲得 2.5 mg/mL (3.77 mM，飽和度未知) 的

4、澄清溶液。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 (3.77 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (3.77 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0

5、 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.77 mM); Clear solution此案可獲得 2.5 mg/mL (3.77 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Nelfinavir Mesylate (AG 1343

6、 Mesylate)種有效的服物可利的 HIV-1 蛋酶抑制劑 (Ki=2 nM) 和抗病毒劑，于治療HIV感染。Nelfinavir Mesylate (AG 1343 Mesylate) 種譜的抗癌劑。IC & Target HIV-1體外研究Nelfinavir (AG1341) Mesylate (1-10 M; 48 hours) inhibits the proliferation of multiple myeloma cells4.Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, im

7、pairs proliferation and triggers apoptosis ofthe myeloma cell lines and fresh plasma cells4.Nelfinavir Mesylate (1-10 M; 17 hours) induces apoptosis of multiple myeloma cell lines4.Nelfinavir Mesylate (5 M; 0-24 hours) decreases the phosphorylation of AKT4.Nelfinavir Mesylate activates the cleavage

8、of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, andactivates the pro-apoptotic pathway of the unfolded protein response system4.Cell Proliferation Assay4Cell Line: RPMI, LP1, U266, OPM2 and MM1S cellsConcentration: 1, 2, 5, 10 MIncubation Time: 48 hoursResult: Inhibited the proli

9、feration of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50 of 1-5 M.Apoptosis Analysis4Cell Line: LP1 and U266 cellsConcentration: 1-10 MIncubation Time: 17 hoursResult: Induced a dose-dependent increase in the percentage of annexin V+/propidiumiodide+ cells.Wester

10、n Blot Analysis4Cell Line: U266 cellsConcentration: 5 MIncubation Time: 0-24 hoursPage 2 of 3 www.MedChemEResult: The level of AKT phosphorylation in U266 cells decreased.體內(nèi)研究 Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCIDmice4.Anim

11、al Model: NOD/SCID mice (bearing U266-luc cells)4Dosage: 75 mg/kgAdministration: I.p.; 5 days a week for 21 daysResult: Decreased MM cell growth in NOD/SCID mice.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Int J Antimicrob Agents. 2019 Dec;54(6):814-819. PLoS One. 2015 Aug 11;10(8):e0134707. bioRxiv. 2020 May.See more customer val

12、idations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Mondal D, et al. Nelfinavir suppresses insulin signaling and nitric oxide production by human aortic endothelial cells: protective effects ofthiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90.2. Kaldor SW, et al. Viracept (nelfinavir me

13、sylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85.3. Gills JJ, et al. Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that inducesendoplasmic reticulum stress, autophagy, andapoptosis in vitro and in vivo. Clin Cancer Res. 2007 Sep 1;13(17):5183-94.4. Bono C, et al. The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiplemyeloma cells in vitro and in vivo. Haematologica. 2012;97(7):1101-1109.McePdfHeightC