Nelfinavir mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服生物可利用的 HIV-1 蛋白酶抑制剂，Ki 为 2 nM；在 HIV-1 株 RF 感染的 CEM-SS 细胞中表现出 30 nM 的抗病毒 EC50。

A potent and orally bioavailable HIV-1 protease inhibitor with Ki of 2 nM; exhibits an antiviral EC50 of 30 nM in HIV-1 strain RF-infected CEM-SS cells; also inhibits the proliferation of NSCLC cells, as well as every cell line in the NCI60 cell line panel with mean GI50 of 5.2 uM, induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo.HIV Infection Approved(In Vitro):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.Nelfinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 35.93 μM.(In Vivo):Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice.

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. Nelfinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 35.93 μM. Cell Proliferation Assay Cell Line:RPMI, LP1, U266, OPM2 and MM1S cells Concentration:1, 2, 5, 10 μMIncubation Time:48 hours Result:Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50 of 1-5 μM. Apoptosis AnalysisCell 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.

Nelfinavir Mesylate (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.

AG-1343 mesylate

Microbiology/Virology

HIV

HIVprotease

Infection

HIV Infection

159989-65-8

663.8881

C33H49N3O7S2

>98% (HPLC)

10 mM in DMSO

CC1=C(C=CC=C1O)C(=O)N[C@@H](CSC2=CC=CC=C2)[C@@H](CN3C[C@H]4CCCC[C@H]4C[C@H]3C(=O)NC(C)(C)C)O.CS(=O)(=O)O

3-Isoquinolinecarboxamide, N-(1,1-dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-, (3S,4aS,8aS)-, methanesulfonate (1:1)

(-20℃)

With Ice Pack

≥ 2 years