Chemical Name: (3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2- hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide methanesulfonate
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Orally active human immunodeficiency virus protease inhibitor. Potently inhibits HIV-1 protease (Ki = 2 nM) in vitro.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
66.39
100
ethanol
66.39
100
Preparing Stock Solutions
The following data is based on the product molecular weight 663.89. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.51 mL
7.53 mL
15.06 mL
5 mM
0.3 mL
1.51 mL
3.01 mL
10 mM
0.15 mL
0.75 mL
1.51 mL
50 mM
0.03 mL
0.15 mL
0.3 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Shettyet al (1996) Preclinical pharmacokinetics and distribution to tissue of AG1343, an inhibitor of human immunodeficiency virus type 1 protease. Antimicrob.Agents Chemother. 40 110 PMID: 8787890
Paticket al (1996) Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob.Agents Chemother. 40 29 PMID: 8787874
Gillset al (2007) Nelfinavir, a lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that induces endoplasmic reticulum stress, autophagy and apoptosis in vitro and in vivo. Clin.Cancer Res. 13 5183 PMID: