Saquinavir

SKU: orb1299397

Description

Saquinavir (Ro 31-8959) is a small molecule HIV-1 protease inhibitor used as an antiretroviral agent. It is widely applied in biochemical research to study viral replication mechanisms and evaluate combination therapies in both cellular and animal models of HIV infection.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Metabolism Research, Pharmacology & Drug Discovery, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 127779-20-8
• MW: 670.84
• Purity: 99.50% (May vary between batches)
• Formula: C₃₈H₅₀N₆O₅
• SMILES: CC(C)(C)NC(=O)C1CC2CCCCC2CN1CC(O)C(Cc1ccccc1)NC(=O)C(CC(N)=O)NC(=O)c1ccc2ccccc2n1
• Target: Calcium Channel,NO Synthase,ROS,HIV Protease,p38 MAPK,Apoptosis,TLR,JNK,Interleukin,SARS-CoV
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (7.45 mM);DMSO:260 mg/mL (387.57 mM)

Bioactivity

• In Vivo:
  The AUC was not affected by grapefruit juice after intravenous administration, but it increased significantly from 76+/-96 (water, mean (s.d.) to 114+/-70 (microg l[-1] h) (grapefruit juice) after oral saquinavir. Similarly, the oral bioavailability of saquinavir increased by a factor of 2 with grapefruit juice (from 0.7% to 1.4%). In contrast, clearance, volume of distribution and elimination half-life of saquinavir were not affected by grapefruit juice. After oral, but not after intravenous administration, the plasma concentration-time curve showed a second peak after lunch irrespective of pretreatment, suggesting enhancement of absorption by food.
  Read more...
• Animal Research:
  After an overnight fast, eight healthy volunteers were treated with either 400 ml grapefruit juice or water before intravenous (12 mg) or oral saquinavir (600 mg) was administered. Serial blood samples were obtained over the following 24 h and standardized meals were served 5 and 10 h after the administration of saquinavir. The plasma concentrations of saquinavir were determined by high-performance liquid chromatography and pharmacokinetic parameters were calculated by routine methods.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ro 31-8959, SARS coronavirus, Saquinavir, SARS-CoV, SARSCoV, inhibit, Inhibitor, Human immunodeficiency virus, HIV, HIVProtease, HIV Protease

Compound Identifiers

PubChem CID

3579812