Size : 10mM(in1mLDMSO)
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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.
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 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
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.
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Telefono : +1 850 650 7790