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。
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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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |
动物实验配方 |