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Nelfinavir Mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nelfinavir Mesylate图片
CAS NO:159989-65-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
Nelfinavir Mesylate (AG 1343 Mesylate) 是一种有效的、可口服的 HIV-1 蛋白酶抑制剂 (Ki=2 nM),用于 HIV 感染。
Cas No.159989-65-8
别名甲磺酸奈非那韦,AG 1343 Mesylate;AG1343 Mesylate;AG-1343 Mesylate,Nelfinavir
化学名(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide;methanesulfonic acid
Canonical SMILESCC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O
分子式C33H49N3O7S2
分子量663.89
溶解度≥ 66.4 mg/mL in DMSO, ≥ 100.4 mg/mL in EtOH with gentle warming
储存条件Store at 2-8℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Nelfinavir Mesylate is a potent inhibitor of HIV-1 protease [1].
HIV-1 protease is a constitutive enzyme that processes gag and gag-pol polyproteins for packaging into the nascent virion actively budding from a productively infected cell. Inhibition of the enzyme results in the formation of immature non-infectious particles [2].
Nelfinavir Mesylate is a potent inhibitor of HIV-1 protease with Ki of 2.0 nM. In CEM cells infected with the HIV strain IIIB, Nelfinavir Mesylate was potent antiviral agent with ED50 value of 14 nM and exhibited minimal cellular toxicity (TD50s > 5000 nM) [1]. In CEM-SS and MT-2 cells, Nelfinavir Mesylate protected these cells from acute HIV-1 RF- and HIV-1 IIIB-induced cell killing with EC50s ranging from 31 to 43 nM [3].
In 65 HIV-1-infected patients, Nelfinavir Mesylate was well-tolerated and exhibited robust antiviral activity with demonstrable superiority of the 750 mg and 1000 mg three times daily regimens. Thirty patients who continued to receive therapy at 12 months acquired a persistent 1.6 log10 reduction in HIV RNA, accompanied by a mean increase in CD4 cells of 180-200/mm3 [2].
References:
[1]. Kaldor SW, Kalish VJ, Davies JF, et al. Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem, 1997, 40(24): 3979-3985.
[2]. Markowitz M, Conant M, Hurley A, et al. A preliminary evaluation of nelfinavir mesylate, an inhibitor of human immunodeficiency virus (HIV)-1 protease, to treat HIV infection. J Infect Dis, 1998, 177(6): 1533-1540.
[3]. Patick AK, Mo H, Markowitz M, et al. Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob Agents Chemother, 1996, 40(2): 292-297.