甲磺酸萘非那韦检测

甲磺酸萘非那韦

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 甲磺酸萘非那韦价格(试剂级) 上下游产品信息中文名称中文同义词英文名称英文同义词CAS号分子式分子量EINECS号相关类别Mol文件结构式

甲磺酸萘非那韦

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

NELFINAVIR

Nelfinavir Regeoisomer;N-tert-butyl-2-[2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)-oxomethyl]amino]-4-(phenylthio)butyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide;AG 1341; AG-1341; AG1341;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

159989-64-7

C32H45N3O4S

567.78

1533716-785-6

peptides

159989-64-7.mol

甲磺酸萘非那韦 性质

熔点沸点比旋光度密度储存条件溶解度形态酸度系数(pKa)颜色水溶解性

185-186 °C

786.8±60.0 °C(Predicted)

D -119.23° (c = 0.26 in methanol)

1.22±0.1 g/cm3(Predicted)

under inert gas (nitrogen or Argon) at 2–8 °C

乙醇中≥20.45mg/mL

粉末

pKa1 6.0; pKa2 11.06(at 25℃)

白色至米白色

7g/L(temperature not stated)

甲磺酸萘非那韦 用途与合成方法

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。靶点

HIV-1

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.