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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

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt663.89
Cas No.159989-65-8
FormulaC33H49N3O7S2
SynonymsAG 1343 Mesylate;AG1343 Mesylate;AG-1343 Mesylate,Nelfinavir
Solubility≥66.4 mg/mL in DMSO; insoluble in H2O; ≥100.4 mg/mL in EtOH with gentle warming
Chemical Name(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
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

甲磺酸奈非那韦(nelfinavir mesylate)是一种有效的HIV-1蛋白酶抑制剂[1].

HIV-1蛋白酶是一种加工gag和gag-pol多聚蛋白的组成酶,将蛋白从有效感染的细胞积极地包装到新生的病毒粒子中.抑制这种酶的活性可导致不成熟的非感染性病毒粒子形成[2].

甲磺酸奈非那韦(nelfinavir mesylate)是一种有效的HIV-1蛋白酶抑制剂,Ki值为 2.0 nM.在HIV株IIIB感染的CEM细胞中,甲磺酸奈非那韦(nelfinavir mesylate)显示出强的抗病毒活性,ED50值为14 nM,以及最小的细胞毒性(TD50s >5000 nM)[1].在CEM-SS和MT-2细胞中,甲磺酸奈非那韦(nelfinavir mesylate)保护这些细胞免于急性HIV-1 RF和HIV-1 IIIB诱导的细胞死亡,EC50s范围从31到43 nM[3].

在65位HIV-1感染的患者中,甲磺酸奈非那韦(nelfinavir mesylate)耐受性良好,并且表现出强大的抗病毒活性,750 mg和1000 mg每日三次的治疗方案显示出明显的优势.在30位持续12个月接受治疗的患者中,可持续减少1.6 log10的HIV RNA,并伴随着平均180-200个/mm3 CD4细胞的增加[2].

参考文献：
[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.

试验操作

Cell experiment:[1]

Cell lines

CEM cells

Reaction Conditions

14 nM nelfinavir mesylate

Applications

In CEM cells infected with the HIV strain IIIB, nelfinavir mesylate was demonstrated to be a potent antiviral agent with ED50 value of 14 nM, and exhibited minimal cellular toxicity (TD50s >5000 nM).

Animal experiment:[1]

Animal models

Male Sprague-Dawley rats, beagle dogs (one male and one female), marmosets (one male and one female) and female cynomolgus monkeys

Dosage form

25 ~ 50 mg/kg

Administered orally

Applications

Nelfinavir mesylate demonstrated significant oral bioavailability across a range of species including rats (43%), dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). In addition, a single oral dose of nelfinavir mesylate exhibited plasma levels exceeding the in vitro antiviral ED95 (58 nM, 40 ng/mL) for more than 6 h in three of the four species. In vivo studies indicate that nelfinavir mesylate is well absorbed orally in a variety of species.

Note

The technical data provided above is for reference only.

References:

1. Kaldor SW, Kalish VJ, Davies JF 2nd, et al. Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. Journal of Medicinal Chemistry, 1997, 40(24): 3979-3985.