159989-65-8
159989-65-8 結(jié)構(gòu)式
基本信息
甲磺酸奈非那韋
甲磺酸萘非那韋
奈非那維
AG-1343
NELFINAVIR MESYLATE
8a-beta))-a-betmonomethanesulfonate(salt)
droxy-2-methylbenzoyl)amino)-4-(phenylthio)butyl)-,(3s-(2(2,s*,3s*),3-alpha,4
viracept
Nelfinavir1
(3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide
NELFINAVIRMESYLATE(SUBJECTTOPATENTFREE)
Nelfinavir nesylate
(3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide mesylate
(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
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法
75-75-2
159989-64-7
159989-65-8
在25-35℃條件下，將甲基磺酸（8.46g，88mmol）緩慢加入至(3S,4aS,8aS)-N-(叔丁基)-2-((2R,3R)-2-羥基-3-(3-羥基-2-甲基苯甲酰胺基)-4-(苯硫基)丁基)十氫異喹啉-3-羧酰胺（50g，88mmol）的丙酮（400ml）懸浮液中，持續(xù)攪拌直至形成澄清溶液。將反應(yīng)混合物于20-25℃下繼續(xù)攪拌2小時，隨后通過過濾收集沉淀產(chǎn)物，并用丙酮（100ml）洗滌。將所得固體在70-75℃下進行減壓干燥，直至失重（LOD）達到-8% w/w，最終獲得57.5g（產(chǎn)率98%）的(3S,4aS,8aS)-N-(叔丁基)-2-((2R,3R)-2-羥基-3-(3-羥基-2-甲基苯甲酰胺)-4-(苯硫基)丁基)十氫異喹啉-3-甲酰胺 甲磺酸鹽，其純度經(jīng)高效液相色譜（HPLC）分析大于99.5%，并通過X射線衍射（XRD）確認其結(jié)晶形態(tài)。
參考文獻：
[1] Patent: WO2008/41087, 2008, A1. Location in patent: Page/Page column 6
[2] Patent: WO2008/41087, 2008, A1. Location in patent: Page/Page column 10-11
[3] Patent: EP1361216, 2003, A1. Location in patent: Page/Page column 30
[4] Patent: WO2006/21964, 2006, A2. Location in patent: Page/Page column 6
[5] Patent: EP1361216, 2003, A1. Location in patent: Page/Page column 30-31
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2025/05/22 | 46620 | 甲磺酸奈非那韋 Nelfinavir mesylate | 159989-65-8 | 250mg | 3207元 |
| 2025/05/22 | 46620 | 甲磺酸奈非那韋 Nelfinavir mesylate | 159989-65-8 | 1g | 11102元 |
| 2025/05/22 | HY-15287A | 甲磺酸奈非那韋 Nelfinavir Mesylate | 159989-65-8 | 5mg | 600元 |
常見問題列表
| 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. |