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159989-64-7

中文名稱 甲磺酸萘非那韋
英文名稱 NELFINAVIR
CAS 159989-64-7
分子式 C32H45N3O4S
分子量 567.78
MOL 文件 159989-64-7.mol
更新日期 2024/10/23 11:53:07
159989-64-7 結(jié)構(gòu)式 159989-64-7 結(jié)構(gòu)式

基本信息

中文別名
奈非那韋
尼非那韋
娜芙維亞
萘非那韋
奈非那韋雜質(zhì)
甲磺酸萘非那韋
2-[(2R,3R)-2-羥基-3-[(3-羥基-2-甲基苯甲酰)氨基]-4-(苯基硫)丁基]-(3S,4aS,8aS)-N-叔丁基十氫異喹啉-3-甲酰胺
英文別名
AG 1341
nefinavir
NELFINAVIR
NELFINAVIR-12
8a-beta))-a-bet
NELFINAVIR USP/EP/BP
Nelfinavir Regeoisomer
AG 1341
AG-1341
AG1341
Nelfinavir & Nelfinavir Mesylate
3-isoquinolinecarboxamide,n-(1,1-dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hy
所屬類別
原料藥:抗病毒類藥

物理化學性質(zhì)

熔點185-186 °C
比旋光度D -119.23° (c = 0.26 in methanol)
沸點786.8±60.0 °C(Predicted)
密度1.22±0.1 g/cm3(Predicted)
儲存條件Keep in dark place,Inert atmosphere,2-8°C
溶解度≥ 20.45mg/mL in Ethanol
酸度系數(shù)(pKa)pKa1 6.0; pKa2 11.06(at 25℃)
形態(tài)Powder
顏色White to off-white
水溶解性7g/L(temperature not stated)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302
毒性rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998.

常見問題列表

生物活性
Nelfinavir (AG-1341) 是一種有效的口服生物可利用的 HIV-1 蛋白酶抑制劑 (Ki=2 nM) 用于 HIV 感染。Nelfinavir (AG-1341) 是一種廣譜的抗癌劑。
靶點

HIV-1

體外研究

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.
體內(nèi)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.
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