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.
Technical Data
| M. Wt | 663.89 |
| Formula | C32H45N3O4S.CH4O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 159989-65-8 |
| PubChem ID | 64142 |
| InChI Key | NQHXCOAXSHGTIA-SKXNDZRYSA-N |
| Smiles | [H][C@]12CCCC[C@]([H])1C[C@@H]([C@@](NC(C)(C)C)=O)N(C[C@@H](O)[C@H](CSC3=CC=CC=C3)NC(C4=C(C)C(O)=CC=C4)=O)C2.CS(=O)(O)=O |
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
References
References are publications that support the products' biological activity.
Shetty et 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
Patick et al (1996) Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob.Agents Chemother. 40 29 PMID: 8787874
Gills et 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:
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