Nelfinavir Mesylate|159989-65-8|(AG 1343 Mesylate)-陌孚医药/Medlife

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Nelfinavir Mesylate (Synonyms: AG 1343 Mesylate)

目录号: PC15638 纯度: ≥98%

CAS No. :159989-65-8

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中文名称	Nelfinavir Mesylate
中文别名	甲磺酸奈非那韦;2-[(2R,3R)-2-羟基-3-[(3-羟基-2-甲基苯甲酰)氨基]-4-(苯基硫)丁基]-(3S,4aS,8aS)-N-叔丁基十氢异喹啉-3-甲酰胺甲磺酸盐;甲磺酸奈非那韦水合物;奈非那韦甲磺酸盐;甲磺酸奈非那韦Nelfinavir mesylate;甲磺酸奈非那韦一水标准品;甲磺酸萘非那韦;奈非那韦甲磺酸;奈非那韦甲磺酸盐水合物;奈非那维
英文名称	Nelfinavir Mesylate
英文别名	Nelfinavir mesylate;(3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide mesylate;Nelfinavir Mesylate Hydrate;(3S,4AS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamidemethanesulf;Nelfinavir;Nelfinavir (mesylate);(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide,methanesulfonic acid;AG 1343 Mesylate;AG-1343 Mesylate;Nelfinavir Methanesulfonate Hydrate;Nelfin;AG-1343;viracept;Nelfinavir1;Nelfinavir nesylate;AG1343 Mesylate;Nelfinavir mesylate, >=98%;Nelfinavir mesilate;Nelfinavir Mesylate [USAN];C32H45N3O4S.CH4O3S;Nelfinavir Methanesulfonate;AG1343;98D603VP8V;AG 1343;Viracept (TN);NFV;DSSTox_CID_10777;DSSTox_RID_79093;DSSTox_GSID_33736;3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phe
Cas No.	159989-65-8
分子式	C₃₃H₄₉N₃O₇S₂
分子量	663.89
包装储存	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (K_i=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.

性状

Solid

IC50 & Target[1][2]

HIV-1

体外研究(In Vitro)

Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells.
Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells.
Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines.
Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT.
Nelfinavir Mesylate activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system.
Nelfinavir is also a SARS-CoV 3CL inhibitor with an IC₅₀ of 35.93 μM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	RPMI, LP1, U266, OPM2 and MM1S cells
Concentration:	1, 2, 5, 10 μM
Incubation Time:	48 hours
Result:	Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC₅₀ of 1-5 μM.

Apoptosis Analysis

Cell Line:	LP1 and U266 cells
Concentration:	1-10 μM
Incubation Time:	17 hours
Result:	Induced a dose-dependent increase in the percentage of annexin V/propidium iodide cells.

Western Blot Analysis

Cell Line:	U266 cells
Concentration:	5 μM
Incubation Time:	0-24 hours
Result:	The level of AKT phosphorylation in U266 cells decreased.

体内研究(In Vivo)

Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mice (bearing U266-luc cells)
Dosage:	75 mg/kg
Administration:	I.p.; 5 days a week for 21 days
Result:	Decreased MM cell growth in NOD/SCID mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Mondal D, et al. Nelfinavir suppresses signaling and nitric oxide production by human aortic endothelial cells: protective effects of thiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90. [Information]

[2]. Gills JJ, et al. Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that inducesendoplasmic reticulum stress, autophagy, and apoptosis 体外研究 and in vivo. Clin Cancer Res. 2007 Sep 1;13(17):5183-94. [Information]

[3]. Kaldor SW, et al. Nelfinavir mesylate (AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85. [Information]

[4]. Bono C, et al. The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiple myeloma cells 体外研究 and in vivo. Haematologica. 2012;97(7):1101‐1109. [Information]

[5]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (150.63 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5063 mL	7.5314 mL	15.0627 mL
5 mM	0.3013 mL	1.5063 mL	3.0125 mL
10 mM	0.1506 mL	0.7531 mL	1.5063 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方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，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (7.53 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (7.53 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (7.53 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.53 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution
5.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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