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甲磺酸奈非那韦 /Nelfinavir Mesylate {[allProObj[0].p_purity_real_show]}

货号:A228436 同义名: AG 1343 Mesylate;Nelfinavir (mesylate)

Nelfinavir Mesylate (AG 1343 Mesylate) 是一种高效、口服可用的HIV-1蛋白酶抑制剂(Ki=2 nM),用于HIV感染,还具有广谱抗癌作用。

Nelfinavir Mesylate 化学结构 CAS号:159989-65-8
Nelfinavir Mesylate 化学结构
CAS号:159989-65-8
Nelfinavir Mesylate 3D分子结构
CAS号:159989-65-8
Nelfinavir Mesylate 化学结构 CAS号:159989-65-8
Nelfinavir Mesylate 3D分子结构 CAS号:159989-65-8
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Nelfinavir Mesylate 纯度/质量文件 产品仅供科研

货号:A228436 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HIV Protease HIV-1 caspid 其他靶点 纯度
Dextran sulfate sodium, mw 40,000 M.W 40000
Vicriviroc maleate 98+%
Rosamultin 97%
Darunavir 98%
Lopinavir ++++

HIV protease, Ki: 1.3 pM

99+%
Chloroquine Autophagy 95%
Amprenavir +

HIV protease, IC50: 14.6 ng/mL

PXR 99%+
NBD-556 99%+
Nelfinavir Mesylate +++

HIV protease, Ki: 2 nM

99%+
Atazanavir Sulfate 98%
Limonin 98%
Saquinavir ++

HIV proteinase, IC50: 2.7 nM

98%
Ritonavir 98%
Azvudine 98%
Lenacapavir ++++

HIV-1 capsid, EC50: 0.1 nM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Nelfinavir Mesylate 生物活性

靶点
  • HIV Protease

    HIV protease, Ki:2 nM

描述 Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Additionally, Nelfinavir Mesylate (AG 1343 Mesylate) exhibits broad-spectrum anticancer activity [1][2][3].
体内研究

In NOD/SCID mice, administration of Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) suppresses the growth of multiple myeloma cells [4].

体外研究

Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) suppresses the proliferation of multiple myeloma cells [4].

The inhibition of 26S chymotrypsin-like proteasome activity by Nelfinavir Mesylate impedes proliferation and induces apoptosis in myeloma cell lines and fresh plasma cells [4].

Exposure to Nelfinavir Mesylate (1-10 μM; 17 hours) triggers apoptosis in multiple myeloma cell lines [4].

Treatment with Nelfinavir Mesylate (5 μM; 0-24 hours) reduces AKT phosphorylation [4].

Nelfinavir Mesylate promotes caspase-3 cleavage, attenuates AKT, STAT-3, ERK1/2 phosphorylation, and activates the pro-apoptotic pathway of the unfolded protein response system [4].

Moreover, Nelfinavir serves as an inhibitor of SARS-CoV 3CLpro with an IC50 of 35.93 μM [5].

Nelfinavir Mesylate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00002411 HIV Infections Not Applicable Completed - -
NCT00000895 Mycobacterium Avium-intracellu... 展开 >>lare Infection HIV Infections 收起 << Not Applicable Completed - -
NCT00122590 HIV Infections Not Applicable Terminated - France ... 展开 >> Service de Medecine Interne Hopital Cochin Paris, France, 75014 收起 <<

Nelfinavir Mesylate 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.

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

[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.

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

[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.

Nelfinavir Mesylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.51mL

0.30mL

0.15mL

7.53mL

1.51mL

0.75mL

15.06mL

3.01mL

1.51mL

Nelfinavir Mesylate 技术信息

CAS号159989-65-8
分子式C33H49N3O7S2
分子量 663.888
别名 AG 1343 Mesylate;Nelfinavir (mesylate);Nelfin;AG-1343
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(158.16 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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