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AdipoGen Life Sciences
Saquinavir . mesylate
70
CHF
CHF 70.00
In stock
AG-CR1-3727-M01010 mgCHF 70.00
AG-CR1-3727-M05050 mgCHF 210.00
| Product Details | |
|---|---|
| Synonyms | Ro 31-8959 |
| Product Type | Chemical |
| Properties | |
| Formula |
C38H50N6O5 . CH4SO3 |
| MW | 670.9 . 96.1 |
| CAS | 149845-06-7 |
| RTECS | EJ6664000 |
| Purity Chemicals | ≥98% |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (10mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | IRHXGOXEBNJUSN-YOXDLBRISA-N |
| Smiles | CS(=O)(O)=O.O[C@@H]([C@@H](NC([C@H](CC(N)=O)NC(C1=NC(C=CC=C2)=C2C=C1)=O)=O)CC3=CC=CC=C3)CN4C[C@@]5([H])CCCC[C@@]5([H])C[C@H]4C(NC(C)(C)C)=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Saquinavir is an antiretroviral inhibitor of the human immunodeficiency virus. It potently inhibits HIV-1 (Ki=0.12nM) and HIV-2 (Ki<0.1nM) protease in vitro. HIV-1 protease is important for the replication of the virus within the cell and the release of mature viral particles from the infected cell.
- Formulations containing saquinavir have been used in combination with other inhibitors for the treatment of AIDS.
- Saquinavir shows other antimicrobial and antiviral activity. Potential SARS-CoV-2 replication inhibitor, responsible for COVID-19.
- Shows anti-cancer activity. Shown to induce apoptosis, autophagy and endoplasmic reticulum stress, which consequently leads to cancer cell death. Inhibits chymotrypsin-like and caspase-like activity of the 26S proteasome and purified 20S proteasome.
- Anti-inflammatory agent. Blocks cathepsin V and thereby inhibits disulfide HMGB1-induced TLR4 activation and cytokine production.
Product References
- Rational design of peptide-based HIV proteinase inhibitors: N.A. Roberts, et al.; Science 248, 358 (1990)
- A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: Synthesis, enzyme inhibition, and antiviral activity: T.J. Tucker, et al.; J. Med. Chem. 35, 2525 (1992)
- Saquinavir: an HIV proteinase inhibitor: K. Bragman; Adv. Exp. Med. Biol. 394, 305 (1996)
- The human immunodeficiency virus (HIV)-1 protease inhibitor saquinavir inhibits proteasome function and causes apoptosis and radiosensitization in non-HIV-associated human cancer cells: F. Pajonk, et al.; Cancer Res. 62, 5230 (2002)
- The HIV protease inhibitors saquinavir, ritonavir, and nelfinavir induce apoptosis and decrease barrier function in human intestinal epithelial cells: H. Bode, et al.; Antivir. Ther. 10, 645 (2005)
- The HIV protease inhibitor saquinavir induces endoplasmic reticulum stress, autophagy, and apoptosis in ovarian cancer cells: K. McLean, et al.; Gynecol. Oncol. 112, 623 (2009)
- Saquinavir, the pioneer antiretroviral protease inhibitor: C.J. la Porte; Expert Opin. Drug Metab. Toxicol. 5, 1313 (2009) (Review)
- Saquinavir inhibits the malaria parasite's chloroquine resistance transporter: R.E. Martin, et al.; Antimicrob. Agents Chemother. 56, 2283 (2012)
- The antiretroviral agent saquinavir enhances hTERT expression and telomerase activity in human T leukaemia cells in vitro: R. Adamo, et al.; J. Exp. Clin. Cancer Res. 32, 38 (2013)
- The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88: J.P. Pribis, et al.; Mol. Med. 21, 749 (2015)
- Saquinavir Ameliorates Liver Warm Ischemia-Reperfusion-Induced Lung Injury via HMGB-1- and P38/JNK-Mediated TLR-4-Dependent Signaling Pathways: Z. Yu, et al.; Mediators Inflamm. 2017, 7083528 (2017)
- A search for medications to treat COVID-19 via in silico molecular docking models of the SARS-CoV-2 spike glycoprotein and 3CL protease: D.C. Hall & H.F. Ji; Travel Med Infect Dis. (Epub ahead of print) (2020)
- Identification of chymotrypsin-like protease inhibitors of SARS-CoV-2 via integrated computational approach: S.A. Khan, et al.; J. Biomol. Struct. Dyn. 39, 2607 (2021)
- Unrevealing sequence and structural features of novel coronavirus using in silico approaches: The main protease as molecular target: J.T. Ortega, et al.; EXCLI J. 19, 400 (2020)
- Identification of FDA Approved Drugs Targeting COVID-19 Virus by Structure-Based Drug Repositioning: P. Wang, et al.; ChemRxiv (Preprint) (2020)
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