A3653-1ml | Nelfinavir Mesylate [159989-65-8] Clinisciences

Background

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.

Product Citation

1. Lili Zhang, Jiaxin Yang, et al. "Enterovirus D68 Infection Induces TDP-43 Cleavage, Aggregation, and Neurotoxicity." J Virol. 2023 Apr 27;97(4):e0042523. PMID: 37039659

Chemical Properties

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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

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.

Quality Control

Purity = 98.04%

Nelfinavir Mesylate [159989-65-8]

Referentie A3653-1ml

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