甲磺酸奈非那韦作用机制 - Medchemexpress - MCE中国

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

2、 unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动

3、物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.77 mM); Clear solution此案可获得 2.5 mg/mL (3.77 mM，饱和度未知) 的

4、澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.77 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (3.77 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0

5、 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.77 mM); Clear solution此案可获得 2.5 mg/mL (3.77 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Nelfinavir Mesylate (AG 1343

6、 Mesylate)种有效的服物可利的 HIV-1 蛋酶抑制剂 (Ki=2 nM) 和抗病毒剂，于治疗HIV感染。Nelfinavir Mesylate (AG 1343 Mesylate) 种谱的抗癌剂。IC & Target HIV-1体外研究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.体内研究 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.户使本产品发表的科研献 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