Nelfinavir
(Synonyms: 萘非那韦,AG1341) 目录号 : GC17709
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
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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]。
| 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: |
|
| Cas No. | 159989-64-7 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | ≥ 20.45mg/mL in Ethanol | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7612 mL | 8.8062 mL | 17.6125 mL |
| 5 mM | 0.3522 mL | 1.7612 mL | 3.5225 mL |
| 10 mM | 0.1761 mL | 0.8806 mL | 1.7612 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet