产品说明书

Nelfinavir

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Chemical Structure| 159989-64-7 同义名 : 奈非那韦 ;AG1341
CAS号 : 159989-64-7
货号 : A128893
分子式 : C32H45N3O4S
纯度 : 99%+
分子量 : 567.782
MDL号 : MFCD01938163
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(184.93 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The HIV-1 protease belongs to the family of aspartyl protease. It cleaves the newly synthesized polyproteins, which is the vital step to create the mature protein components of an infectious HIV-1 virus[3]. Nelfinavir is a selective, nonpeptidic competitive inhibitor of the HIV-1 protease{{Kaldor SW, Kalish VJ, Davies JF II, et al. Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem 1997 Nov 21; 40: 3979-85.|https://pubmed.ncbi.nlm.nih.gov/9397180/}}. Nelfinavir has an in vitro inhibition constant(Ki) of 1.7 nM against HIV-1 protease, but no significant activity against human aspartic proteases including pepsin, renin and gastricin. Very weak affinity for cathepsin E (74 μM) and cathepsin D (435 nM) has been observed. The mean nelfinavir concentration producing 95% inhibition of viral replication (IC95) in a variety of i in vitro HIV infection models was 59 nM (range 7 to 130 nM). Nelfinavir was also effective at inhibiting replication of the zidovudine-resistant HIV-1 strain G910-6 and the NNRTI-resistant strain A17[4]. The mean plasma nelfinavir concentration exceeded the 95% antiviral effective dose (ED95 =40 μg/L) for up to 8 hours after a single 100mg dose, and up to 24 hours after an 800mg dose. The area under the concentration-time curve (AUC) after administration in the fasted state was 27 to 50% of the AUC when the drug was administered with food[5]. Nelfinavir is metabolised in the liver by the cytochrome P450 (CYP) enzyme system. Nelfinavir is metabolically converted to its major hydroxy-t-butylamide metabolite M8, which has anti-HIV activity comparable to nelfinavir i in vitro [6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00624195 HIV Infections Phase 2 Phase 3 Completed - United States, California ... 展开 >> HIV Neurobehavioral Research Center, University of California San Diego San Diego, California, United States, 92103 University of California, San Francisco San Francisco, California, United States, 94110 United States, Maryland Johns Hopkins University- School of Medicine Baltimore, Maryland, United States, 21287 United States, Missouri Washington University St. Louis, Missouri, United States, 63110 United States, New York Mount Sinai Medical Center New York, New York, United States, 10024 收起 <<
NCT00002411 HIV Infections Not Applicable Completed - -
NCT00624195 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.81mL

1.76mL

0.88mL

17.61mL

3.52mL

1.76mL
参考文献

[1]Mondal D, Liu K, et al. Nelfinavir suppresses insulin signaling and nitric oxide production by human aortic endothelial cells: protective effects of thiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90.

[2]Kaldor SW, Kalish VJ, et al. Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85.

[3]Davies, D. R. The structure and function of the aspartic proteinases. Annu. Rev. Biophys. Biophys. Chem. 19, 189–215,

[4]A K Patick,et al. Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob Agents Chemother.1996 Feb;40(2):292-7.

[5]Caroline M Perry,et al. Nelfinavir: a review of its use in the management of HIV infection. Drugs.2005;65(15):2209-44.

[6]A Bardsley-Elliot,et al. Nelfinavir: an update on its use in HIV infection. Drugs. 2000 Mar;59(3):581-620.