甲磺酸奈非那韦

生物活性靶点体外研究体内研究甲磺酸奈非那韦试剂级价格

甲磺酸奈非那韦

CAS号:159989-65-8
英文名:Nelfinavir mesylate
中文名:甲磺酸奈非那韦
CBNumber:CB5213805
分子式:C33H49N3O7S2
分子量:663.89
MOL File:159989-65-8.mol

甲磺酸奈非那韦化学性质

熔点 :131-135°C
储存条件 :Keep in dark place,Inert atmosphere,2-8°C
溶解度 :DMSO: ≥2mg/mL
酸度系数(pKa) :pKa -1.20(at 25℃)
形态 :powder
颜色 :white to off-white
水溶解性 :4.5g/L(temperature not stated)
Merck :14,6443
BCS Class :2,4
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
InChIKey :NQHXCOAXSHGTIA-SKXNDZRYSA-N
CAS 数据库 :159989-65-8(CAS DataBase Reference)

安全信息

WGK Germany :3
RTECS号 :NW6995333
海关编码 :29334900
毒害物质数据 :159989-65-8(Hazardous Substances Data)

甲磺酸奈非那韦性质、用途与生产工艺

生物活性 Nelfinavir Mesylate (Viracept, AG1343) 是强效的HIV protease抑制剂，Ki为2 nM。
靶点
Target Value
HIV protease
(Cell-free assay) 2 nM(Ki)

体外研究

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.

体内研究体内研究表明AG1343在多个物种口服后能很好地被吸收，在人类中具有良好的药代动力学特征。在饲养大鼠中，该化合物的口服生物利用度为43%，而在禁食大鼠中，口服生物利用度显著下降至29%。在多种生物体内，Nelfinavir的生物口服利用度为：犬类中47%、狨猴中17%、食蟹猴中26%。在口服后，其在血浆中半衰期较长，这可能是因为分解和吸收较慢的缘故。在人类中，Nelfinavir能很好地被吸收，尤其是随食物给药时，具有比较少、容易处理的副作用，安全性良好。
用途用作抗病毒药
用途 HIV蛋白酶抑制剂