甲磺酸奈非那韦
| 中文名称 | 甲磺酸奈非那韦 |
|---|---|
| 中文同义词 | 甲磺酸奈非那韦水合物;甲磺酸奈非那韦;奈非那韦甲磺酸盐;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-甲酰胺甲磺酸盐;奈非那维;甲磺酸萘非那韦;(3S,4AS,8AS)-N-(叔丁基)-2-((2R,3R)-2-羟基-3-(3-羟基-2-甲基苯甲酰胺)-4-(苯硫基)丁基)十氢异喹啉-3-甲酰胺 甲磺酸盐;奈非那韦甲磺酸盐一水合物 |
| 英文名称 | Nelfinavir mesylate |
| 英文同义词 | Nelfinavir mesylate, >=98%;Nelfinavir methanesulfonate hydrate;Nelfinavir mesylate hydrate;N-(1,1-dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-(3S,4aS,8aS)-3-isoquinolinecarboxamide, methanesulfonate (1:1);(3S,4aS,8aS)-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methyl-benzoyl)amino]-4-phenylsulfanyl-butyl]-N-tert-butyl-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide;Nelfinavir1;AG-1343 Mesylate;AG1343 Mesylate |
| CAS号 | 159989-65-8 |
| 分子式 | C33H49N3O7S2 |
| 分子量 | 663.89 |
| EINECS号 | |
| 相关类别 | 细胞信号和神经生物学;小分子抑制剂，天然产物;生物活性小分子;标准品;生物活性分子-API;医药原料药 |
| Mol文件 | 159989-65-8.mol |
| 结构式 |  |
甲磺酸奈非那韦 性质
| 熔点 | 131-135°C |
|---|---|
| 储存条件 | Keep in dark place,Inert atmosphere,2-8°C |
| 溶解度 | 二甲基亚砜：≥2mg/mL |
| 酸度系数(pKa) | pKa -1.20(at 25℃) |
| 形态 | 粉末 |
| 颜色 | 白色至类白色 |
| 水溶解性 | 4.5g/L(temperature not stated) |
| Merck | 14,6443 |
| BCS Class | 2,4 |
| 稳定性 | DMSO中的溶液可在-20°下稳定储存3个月。 |
| InChIKey | NQHXCOAXSHGTIA-SKXNDZRYSA-N |
| CAS 数据库 | 159989-65-8(CAS DataBase Reference) |
| Target | Value |
|
HIV protease
(Cell-free assay) | 2 nM(Ki) |
Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells.
Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells.
Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines.
Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT.
Nelfinavir Mesylate 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. |
安全信息
| WGK Germany | 3 |
|---|---|
| RTECS号 | NW6995333 |
| 海关编码 | 29334900 |
| 毒害物质数据 | 159989-65-8(Hazardous Substances Data) |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15287A | 甲磺酸奈非那韦 Nelfinavir Mesylate | 159989-65-8 | 5mg | 600元 |
| 2024/01/25 | HY-15287A | 甲磺酸奈非那韦 Nelfinavir Mesylate | 159989-65-8 | 10mM * 1mLin DMSO | 880元 |