甲磺酸萘非那韦
- CAS号:159989-64-7
- 英文名:NELFINAVIR
- 中文名:甲磺酸萘非那韦
- CBNumber:CB8213806
- 分子式:C32H45N3O4S
- 分子量:567.78
- MOL File:159989-64-7.mol
- 熔点 :185-186 °C
- 沸点 :786.8±60.0 °C(Predicted)
- 比旋光度 :D -119.23° (c = 0.26 in methanol)
- 密度 :1.22±0.1 g/cm3(Predicted)
- 储存条件 :under inert gas (nitrogen or Argon) at 2–8 °C
- 溶解度 :≥ 20.45mg/mL in Ethanol
- 形态 :Powder
- 酸度系数(pKa) :pKa1 6.0; pKa2 11.06(at 25℃)
- 颜色 :White to off-white
- 水溶解性 :7g/L(temperature not stated)
- 毒性 :rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998.
甲磺酸萘非那韦性质、用途与生产工艺
- 生物活性 Nelfinavir (AG-1341) 是一种有效的口服生物可利用的 HIV-1 蛋白酶抑制剂 (Ki=2 nM) 用于 HIV 感染。Nelfinavir (AG-1341) 是一种广谱的抗癌剂。
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靶点
HIV-1
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体外研究
Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells.
Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells.
Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines.
Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT.
Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system.Cell Proliferation Assay
Cell Line: RPMI, LP1, U266, OPM2 and MM1S cells Concentration: 1, 2, 5, 10 μM Incubation Time: 48 hours Result: Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC 50 of 1-5 μM. Apoptosis Analysis
Cell Line: LP1 and U266 cells Concentration: 1-10 μM Incubation Time: 17 hours Result: Induced a dose-dependent increase in the percentage of annexin V + /propidium iodide + cells. Western Blot Analysis
Cell Line: U266 cells Concentration: 5 μM Incubation Time: 0-24 hours Result: The level of AKT phosphorylation in U266 cells decreased. -
体内研究
Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice.
Animal Model: NOD/SCID mice (bearing U266-luc cells) Dosage: 75 mg/kg Administration: I.p.; 5 days a week for 21 days Result: Decreased MM cell growth in NOD/SCID mice.
- 更新日期:2024/11/08
- 产品编号:HY-15287
- 产品名称:Nelfinavir
- CAS编号:
- 包装:1 mg
- 价格:380元
- 更新日期:2024/11/08
- 产品编号:HY-15287
- 产品名称:甲磺酸萘非那韦 Nelfinavir
- CAS编号:159989-64-7
- 包装:2mg
- 价格:600元
- 公司名称:Axon Medchem BV
- 联系电话:--
- 电子邮件:info@axonmedchem.com
- 国家:荷兰
- 产品数:477
- 优势度:30