奈非那韦 Nelfinavir CAS#:159989-64-7

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奈非那韦

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CAS号：159989-64-7 | 英文名称：Nelfinavir

分子式 C₃₂H₄₅N₃O₄S

分子量 568

EINECS号 1533716-785-6

MDL MFCD01938163

Smiles

InChIKey

乙二醇化学百科

基本信息

中文名称	甲磺酸萘非那韦
英文名称	NELFINAVIR
CAS号	159989-64-7
分子式	C32H45N3O4S
分子量	567.78
EINECS号	1533716-785-6

物化性质

熔点	185-186 °C
比旋光度	D -119.23° (c = 0.26 in methanol)
沸点	786.8±60.0 °C(Predicted)
密度	1.22±0.1 g/cm3(Predicted)
溶解度	乙醇中≥20.45mg/mL
形态	粉末
酸度系数(pKa)	pKa1 6.0; pKa2 11.06(at 25℃)
颜色	白色至米白色
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.

生产及用途

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.

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