甲磺酸萘非那韦

生物活性靶点体外研究体内研究甲磺酸萘非那韦试剂级价格

甲磺酸萘非那韦

CAS号:159989-64-7
英文名:NELFINAVIR
中文名:甲磺酸萘非那韦
CBNumber:CB8213806
分子式:C32H45N3O4S
分子量:567.78
MOL File:159989-64-7.mol

甲磺酸萘非那韦化学性质

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 :≥ 20.45mg/mL in Ethanol
形态 :Powder
酸度系数(pKa) :pKa1 6.0; pKa2 11.06(at 25℃)
水溶解性 :7g/L(temperature not stated)

安全信息

毒性 :rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998.

甲磺酸萘非那韦性质、用途与生产工艺

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.