Nelfinavir Mesylate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 663.89 |
| Cas No. | 159989-65-8 |
| Formula | C33H49N3O7S2 |
| Synonyms | AG 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1=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 | 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。 |
| Cell experiment:[1] | |
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Cell lines |
CEM cells |
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Reaction Conditions |
14 nM nelfinavir mesylate |
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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] | |
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Animal models |
Male Sprague-Dawley rats, beagle dogs (one male and one female), marmosets (one male and one female) and female cynomolgus monkeys |
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Dosage form |
25 ~ 50 mg/kg Administered orally |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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质量控制和MSDS
- 批次:
化学结构
