甲磺酸萘非那韦
| 中文名称 | 甲磺酸萘非那韦 |
|---|---|
| 中文同义词 | 甲磺酸萘非那韦;娜芙维亚;尼非那韦;奈非那韦;2-[(2R,3R)-2-羟基-3-[(3-羟基-2-甲基苯甲酰)氨基]-4-(苯基硫)丁基]-(3S,4aS,8aS)-N-叔丁基十氢异喹啉-3-甲酰胺;奈非那韦杂质;萘非那韦;(3S,4AS,8AS)-N-(叔丁基)-2-((2R,3R)-2-羟基-3-(3-羟基-2-甲基苯甲酰胺基)-4-(苯硫基)丁基)十氢异喹啉-3-羧酰胺 |
| 英文名称 | NELFINAVIR |
| 英文同义词 | 3-isoquinolinecarboxamide,n-(1,1-dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hy;8a-beta))-a-bet;nefinavir;NELFINAVIR;(3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide;Nelfinavir & Nelfinavir Mesylate;AG 1341;NELFINAVIR-12 |
| CAS号 | 159989-64-7 |
| 分子式 | C32H45N3O4S |
| 分子量 | 567.78 |
| EINECS号 | 1533716-785-6 |
| 相关类别 | peptides |
| Mol文件 | 159989-64-7.mol |
| 结构式 |  |
甲磺酸萘非那韦 性质
| 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 | 乙醇中≥20.45mg/mL |
| 形态 | 粉末 |
| 酸度系数(pKa) | pKa1 6.0; pKa2 11.06(at 25℃) |
| 水溶解性 | 7g/L(temperature not stated) |
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HIV-1
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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. |
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. |
安全信息
| 毒性 | rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998. |
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15287 | Nelfinavir | 1 mg | 380元 | |
| 2024/01/25 | HY-15287 | 甲磺酸萘非那韦 Nelfinavir | 159989-64-7 | 2mg | 600元 |