Presatovir

SKU: orb1296215

Description

Presatovir (GS-5806) is an orally administered small molecule fusion inhibitor targeting respiratory syncytial virus (RSV), demonstrating potent antiviral activity with a mean EC50 of 0.43 nM. It has been utilized in both in vitro virology studies and in vivo preclinical models to investigate RSV infection and therapeutic intervention.

Research Area

Infectious Disease & Virology

Key Properties

• CAS Number: 1353625-73-6
• MW: 532.06
• Purity: 99.92% (May vary between batches)
• Formula: C₂₄H₃₀ClN₇O₃S
• SMILES: Cc1cn2nc(cc2nc1N1CC[C@H](N)C1)[C@@H]1CCCCN1C(=O)c1cc(Cl)ccc1NS(C)(=O)=O
• Target: RSV
• Solubility: DMSO:1 mg/mL (1.88 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  RSV:0.43 nM (EC50)
• In Vivo:
  In a cotton rat model of RSV infection, Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy. Oral bioavailability in preclinical species ranges from 46 to 100%, with penetration of the compound into the lung tissue demonstrated in Sprague-Dawley rats. Multidose oral treatment of Presatovir appears safe in adults, and in healthy human volunteers experimentally infected with RSV, a potent antiviral effect and reduction in disease severity are observed in the high dose group .
  Read more...
• In Vitro:
  Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates (mean EC50: 0.43 nM) . GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity .
  Read more...
• Cell Research:
  GS-5806 is diluted in 100% DMSO. To conduct the cytopathic antiviral assay, 0.4 μL of 100×concentrated 3-fold serially diluted drug is added to 20 μL of cell culture medium in a 384-well plate. HEp-2 cells are then suspended in MEM plus 10% FBS at a density of 1×10^5 cells/mL, are infected in bulk with RSV A2 at a titer of approximately 1×10^4.5 tissue culture infectious doses/mL. Immediately following infection, 20 μL of RSV-infected cells are added to each well. The cells are then cultured for 4 days at 37 °C. Following this incubation, the cells are allowed to equilibrate to 25°C. The RSV-induced cytopathic effect is determined by adding 40 μL of Cell-Titer Glo viability reagent. Following a 10 min incubation at 25 °C, cell viability is determined .
  Read more...

Storage & Handling

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

Alternative Names

Inhibitor, GS 5806, GS5806, GS-5806, inhibit, Presatovir, RSV, Respiratory syncytial virus

Compound Identifiers

PubChem CID

58029842