Nelfinavir

目录号: GC17709纯度: >99.00%同义词: 萘非那韦,AG1341

Nelfinavir是一种选择性的、非肽类的HIV-1蛋白酶竞争性抑制剂。Nelfinavir对HIV-1病毒株显示出良好的体外活性。

Cas No.: 159989-64-7

规格	价格	库存	数量
2mg	¥540.00	现货	1
5mg	¥990.00	现货	1
10mg	¥1,485.00	现货	1
50mg	¥3,420.00	现货	1
10mM (in 1mL DMSO)	¥1,237.00	现货	1

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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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388(6745) (2025)
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产品描述 Description

Nelfinavir is a selective, nonpeptidic competitive inhibitor of HIV-1 protease. Nelfinavir shows good in vitro activity against HIV-1 strains^[1].

In vitro, Nelfinavir (1, 2.5, 5, 10, 20, 40 and 60µM; 24 and 48h) dose-dependently suppressed proliferation of human A549 cells^[2]. Nelfinavir (20μM; 24h) can directly inhibit the activity of aspartic protease DNA damage inducible 1 homolog 2 (DDI2), thereby effectively blocking the proteolysis of NFE2L1 and enhancing the cytotoxicity of proteasome inhibitors (PIs) in cancer cells^[3].

In vivo, combining Nelfinavir (50mg/kg/daily; 13 days; i.p.) with Chloroquine inhibits in vivo growth of human lung cancer xenograft tumors^[4]. Nelfinavir (100mg/kg per day; 24 days; i.p.) and metformin, when used in combination, act synergistically to inhibit the growth of cervical cancer cell xenografts in nude mice^[5].

References:
[1] Perry CM, Frampton JE, McCormack PL, Siddiqui MA, Cvetković RS. Nelfinavir: a review of its use in the management of HIV infection. Drugs. 2005;65(15):2209-44.
[2] He F, Wang G, Xu Z, Huang Z. Nelfinavir restricts A549 cell growth by inhibiting STAT3 signaling. J Int Med Res. 2021 Jun;49(6):3000605211014989.
[3] Gu Y, Wang X, Wang Y, Wang Y, Li J, Yu FX. Nelfinavir inhibits human DDI2 and potentiates cytotoxicity of proteasome inhibitors. Cell Signal. 2020 Nov;75:109775.
[4] Lopiccolo J, Kawabata S, Gills JJ, Dennis PA. Combining Nelfinavir With Chloroquine Inhibits In Vivo Growth of Human Lung Cancer Xenograft Tumors. In Vivo. 2021 Jan-Feb;35(1):141-145.
[5] Xia C, Chen R, Chen J, Qi Q, Pan Y, Du L, Xiao G, Jiang S. Combining metformin and nelfinavir exhibits synergistic effects against the growth of human cervical cancer cells and xenograft in nude mice. Sci Rep. 2017 Mar 2;7:43373.

Nelfinavir是一种选择性的、非肽类的HIV-1蛋白酶竞争性抑制剂。Nelfinavir对HIV-1病毒株显示出良好的体外活性^[1]。

在体外实验中，Nelfinavir (1, 2.5, 5, 10, 20, 40和60µM; 24小时和48小时)以剂量依赖性方式抑制人A549细胞的增殖^[2]。Nelfinavir (20µM; 24小时)能够直接抑制天冬氨酸蛋白酶DNA损伤诱导蛋白1同源物2(DDI2)的活性，从而有效阻断NFE2L1的蛋白降解，并增强蛋白酶体抑制剂(PIs)在癌细胞中的细胞毒性^[3]。

在体内实验中，Nelfinavir (50mg/kg/每天; 13天; 腹腔注射)与氯喹联合使用能够抑制人肺癌异种移植物肿瘤的体内生长^[4]。Nelfinavir (100mg/kg/每天; 24天; 腹腔注射)与二甲双胍联合使用时，能够协同抑制裸鼠中宫颈癌细胞异种移植物的生长^[5]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:
Cell lines	A549 and H1224
Preparation Method	Human A549 cells were plated in 96-well plates at a density of 8000 cells per well and cultured overnight at 37°C. The next days, cells were treated with different concentrations of Nelfinavir (1, 2.5, 5, 10, 20, 40 and 60µM) for 24 and 48 hours. MTT reagent was added to each well and incubated for 4 hours at 37°C. The formazan crystals formed by the reduction of MTT by mitochondrial succinic dehydrogenase secreted by viable cells were dissolved using 150µL of DMSO. Absorbance was measured at 490nm. The experiment was repeated using H1224 cells.
Reaction Conditions	1, 2.5, 5, 10, 20, 40 and 60µM; 24 and 48 hours
Applications	Nelfinavir dose-dependently suppressed proliferation of human A549 cells.
Animal experiment [2]:
Animal models	6-week-old female athymic NCr-nu/nu mice
Preparation Method	Cells (5×10⁶ H157 or H549) were suspended in 100µL of phosphate-buffered saline and subcutaneously injected into the bilateral rear flanks of 6-week-old female athymic NCr-nu/nu mice. When the transplanted tumors reached a volume of 50mm³, the mice were divided into four groups (5 mice per group): (i) Vehicle control (4% DMSO, 5% polyethylene glycol, 5% Tween 80 in saline); (ii) 50mg/kg Nelfinavir; (iii) 50mg/kg chloroquine; or (iv) the combination of Nelfinavir and chloroquine, with intraperitoneal injection once daily for 13 days. The body weights of the animals and the sizes of the tumors were measured every other day. In all studies, tumor volume was calculated using the formula v=(ab²)/2, where a and b represent the long axis and short axis of the tumor, respectively. Immunoblotting analysis was performed to detect markers of apoptosis and endoplasmic reticulum (ER) stress.
Dosage form	50mg/kg/daily; 13 days; i.p.
Applications	Combining Nelfinavir with Chloroquine inhibits in vivo growth of human lung cancer xenograft tumors
References: [1] He F, Wang G, Xu Z, Huang Z. Nelfinavir restricts A549 cell growth by inhibiting STAT3 signaling. J Int Med Res. 2021 Jun;49(6):3000605211014989. [2] Lopiccolo J, Kawabata S, Gills JJ, Dennis PA. Combining Nelfinavir With Chloroquine Inhibits In Vivo Growth of Human Lung Cancer Xenograft Tumors. In Vivo. 2021 Jan-Feb;35(1):141-145.

产品文档 Product Documents

批次：Purity:>99.00%

化学性质Chemical Properties

CAS 号

159989-64-7

同义词

萘非那韦,AG1341

化学名

(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

SMILES

CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O

分子式

C₃₂H₄₅N₃O₄S

分子量

567.78 g/mol

溶解性

≥ 20.45mg/mL in Ethanol

保存条件

Store at -20°C

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储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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