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Amprenavir (agenerase)HIV-1 protease inhibitor

Amprenavir (agenerase)

Catalog No. A8201
Size Price Stock Qty
10mM (in 1mL DMSO) $78.00 In stock
Evaluation Sample $28.00 In stock
5mg $45.00 In stock
50mg $310.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Amprenavir(agenerase)

Related Biological Data

Amprenavir(agenerase)

Related Biological Data

Amprenavir(agenerase)

Biological Activity

Description Amprenavir is an inhibitor of HIV protease with IC50 of 14.6 ng/mL in wild-type HIV isolates.
Targets HIV Protease          
IC50            

Protocol

Cell experiment [1]:

Cell lines

HepaRG hepatoma cells and LS180 intestinal cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

10 μM; 24 hrs

Applications

Amprenavir induced PXR target gene expression in both HepaRG hepatoma cells and LS180 intestinal cells.

Animal experiment [1]:

Animal models

WT and PXR-/- mice

Dosage form

10 mg/kg; p.o.; for 1 week

Applications

In the intestine of WT mice, Amprenavir-mediated PXR activation stimulated the expression of both LipF and LipA.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Helsley RN, Sui Y, Ai N, Park SH, Welsh WJ, Zhou C. Pregnane X receptor mediates dyslipidemia induced by the HIV protease inhibitor amprenavir in mice. Mol Pharmacol. 2013 Jun;83(6):1190-9.

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Chemical Properties

Cas No. 161814-49-9 SDF Download SDF
Chemical Name [(3S)-oxolan-3-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
Canonical SMILES CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N
Formula C25H35N3O6S M.Wt 505.63
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips No
Shipping Condition No

Background

Amprenavir (agenerase), an N,N-disubstituted hydroxyethylamino sulfonamide, is a novel inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that potently inhibits the activity of HIV-1 protease with a value of 50% inhibition concentration IC50 of 0.6 nM and also weakly inhibits HIV-2 protease with IC50 value of 19 nM. Amprenavir binds to the catalytic aspartate residues of the HIV-1 protease and hence inhibits the processing of the gag and gag-pol polyprotein precursors, which cleave to yield structural proteins and replication enzymes of HIV, resulting in immature and noninfectious viral particles. Amprenavir has been effectively used for the treatment of HIV disease in patients with primary HIV infection.

Reference

Fung HB, Kirschenbaum HL, Hameed R. Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor. Clin Ther. 2000 May;22(5):549-72.