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/ Nelfinavir Mesylate/甲磺酸奈非那韦

Nelfinavir Mesylate/甲磺酸奈非那韦 {[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/甲磺酸奈非那韦 化学结构 CAS号：159989-65-8
Nelfinavir Mesylate/甲磺酸奈非那韦 化学结构
CAS号：159989-65-8
Nelfinavir Mesylate/甲磺酸奈非那韦 3D分子结构
CAS号：159989-65-8
Nelfinavir Mesylate/甲磺酸奈非那韦 化学结构 CAS号：159989-65-8
Nelfinavir Mesylate/甲磺酸奈非那韦 3D分子结构 CAS号：159989-65-8
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Nelfinavir Mesylate/甲磺酸奈非那韦 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]}
批次查询： 批次纯度:

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产品名称 HIV Protease ↓ HIV-1 caspid ↓ 其他靶点 纯度
Dextran sulfate sodium salt(MW 40000) ✔ M.W 40000
Vicriviroc maleate ✔ 95%
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/甲磺酸奈非那韦 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/甲磺酸奈非那韦 细胞实验

Cell Line
Concentration Treated Time Description References
T-ALL cells 1-20 µM 16 hours To evaluate the cytotoxicity; nelfinavir decreased the percentage of viable cells in a dose-dependent manner compared with DMSO treatment. Int J Oncol. 2023 Nov;63(5):128.
E. multilocularis metacestode vesicles 40 µM 3 and 7 days To evaluate the efficacy of Nelfinavir on E. multilocularis metacestode vesicles, results showed that Nelfinavir significantly increased mortality of PSCs within the cysts. EBioMedicine. 2022 Aug;82:104177.
Human neutrophils 20 or 50 μg/ml 45 min To assess the effect of Nelfinavir on the migration of neutrophils towards the chemokine CXCL8; it was observed that Nelfinavir enhanced neutrophil migration. Antiviral Res. 2022 Jun;202:105311.
ME-180 cells 10 µM 48 hours To evaluate the inhibitory effect of Nelfinavir on the growth of cervical cancer cells, results showed that Nelfinavir significantly inhibited the growth of ME-180 cells. Drug Des Devel Ther. 2016 Jun 2;10:1837-46.
ME-180 CPR cells 10 µM 48 hours To evaluate the inhibitory effect of Nelfinavir on the growth of cisplatin-resistant cervical cancer cells, results showed that Nelfinavir significantly inhibited the growth of ME-180 CPR cells. Drug Des Devel Ther. 2016 Jun 2;10:1837-46.
A549 cells 1.25 µM 72 hours Nelfinavir Mesylate inhibits HAdV-C2 multi-round plaque formation, but not single round infection. Sci Data. 2020 Aug 12;7(1):265.
E. multilocularis protoscoleces (PSCs) 40 µM 72 hours To evaluate the protoscolicidal effect of Nelfinavir on E. multilocularis PSCs, results showed that Nelfinavir significantly increased mortality and reduced viability of PSCs. EBioMedicine. 2022 Aug;82:104177.

Nelfinavir Mesylate/甲磺酸奈非那韦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice SCL-LMO1 transgenic mouse model Intraperitoneal injection 100 mg/kg Daily for 2 weeks To confirm the efficacy of nelfinavir; mice treated with nelfinavir exhibited a mean 68% reduction in tumor burden. Int J Oncol. 2023 Nov;63(5):128.
Nude mice Cervical cancer model Gastric gavage 250 mg/kg/day Once daily for 21 days To evaluate the inhibitory effect of Nelfinavir on tumor growth in vivo, results showed that Nelfinavir significantly inhibited tumor growth. Drug Des Devel Ther. 2016 Jun 2;10:1837-46.
Syrian hamsters Covid-19 infection model Intraperitoneal injection 50 mg/kg Twice daily for four consecutive days To evaluate the effect of Nelfinavir on lung pathology in SARS-CoV-2-infected hamsters; Nelfinavir significantly improved lung pathology despite lack of antiviral efficacy. Antiviral Res. 2022 Jun;202:105311.
Mice E. multilocularis PSC-infected BALB/c mice Oral 50 mg/kg/day Once daily for 28 days To evaluate the efficacy of Nelfinavir in E. multilocularis-infected mice, results showed that Nelfinavir significantly reduced parasite burden (weight of cysts). EBioMedicine. 2022 Aug;82:104177.

Nelfinavir Mesylate/甲磺酸奈非那韦 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/甲磺酸奈非那韦 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/甲磺酸奈非那韦 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/甲磺酸奈非那韦 技术信息

CAS号159989-65-8
分子式C33H49N3O7S2
分子量 663.89
SMILES Code O=C([C@H]1N(C[C@@H](O)[C@@H](NC(C2=CC=CC(O)=C2C)=O)CSC3=CC=CC=C3)C[C@@]4([H])CCCC[C@@]4([H])C1)NC(C)(C)C.OS(=O)(C)=O
MDL No. MFCD00931436
别名 AG 1343 Mesylate; Nelfinavir (mesylate); Nelfin; AG-1343
运输蓝冰
InChI Key NQHXCOAXSHGTIA-SKXNDZRYSA-N
Pubchem ID 64142
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
方案 四
方案 五
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案 一

Tags: Nelfinavir | 159989-65-8 | AG 1343 | AG1343 | AG-1343 | HIV-1 Protease Inhibitor | Metabolic Enzyme/Protease | Anti-infection | HIV Protease | HIV | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Nelfinavir Mesylate/甲磺酸奈非那韦 纯度/质量文件 | Nelfinavir Mesylate/甲磺酸奈非那韦 亚型比较 | Nelfinavir Mesylate/甲磺酸奈非那韦 生物活性 | Nelfinavir Mesylate/甲磺酸奈非那韦 临床数据 | Nelfinavir Mesylate/甲磺酸奈非那韦 参考文献 | Nelfinavir Mesylate/甲磺酸奈非那韦 实验方案 | Nelfinavir Mesylate/甲磺酸奈非那韦 技术信息

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