Saquinavir is a decahydroisoquinoline-based, selective inhibitor of aspartic protease encoded by HIV with an IC50 range of 0.5-6.0 nM and IC90 range of 6.0-30.0 nM. [1] Binding inhibition constants for saquinavir against HIV-1 and HIV-2 are 0.12 nM and
Antiviral potency of saquinavir were shown in JM cells infected with HIV-1 strain GB8 with a IC50 of 2.5 nM. [2] Similarly, and IC50 of 2 nM was obtained against HIV-1 (strain RF) in C8166 cells.
Saquinavir was shown to be a substrate for P-glycoprotein transporter protein, affecting intracellular concentrations and bioavailability. [3]
Technical information:
| Chemical Formula: | C38H50N6O5 | |
| CAS #: | 127779-20-8 | |
| Molecular Weight: | 670.84 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | (2S)-N-[(2S,3R)-4-[(3S)-3-(tert-butylcarbamoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinolin-2-ylformamido)butanediamide | |
| Solubility: | Up to 22 mM in DMSO | |
| Synonyms: | RO318959, RO-31-8959, saguinavir, Fortovase, Invirase |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Craig et al., Antiviral properties of Ro 31-8959, an inhibitor of human immunodeficiency virus (HIV) proteinase. Anvitiral Res. 1991, 16, 295-395. Pubmed ID: 1810306 |
| 2. | Roberts et al., Rational design of peptide-based HIV proteinase inhibitors. Science, 1990, 248, 358-361. Pubmed ID: 2183354 |
| 3. | Kim et al., Saquinavir, an HIV protease inhibitor, is transported by P-glycoprotein. J. Pharmacol. Exp. Ther. 1998, 286(3), 1439-1445. Pubmed ID: 9732409 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
