1. Anti-infection
  2. RSV

Presatovir (Synonyms: GS-5806)

Cat. No.: HY-16727 Purity: 99.48%
Handling Instructions

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.

For research use only. We do not sell to patients.
Presatovir Chemical Structure

Presatovir Chemical Structure

CAS No. : 1353625-73-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 492 In-stock
5 mg USD 420 In-stock
10 mg USD 720 In-stock
50 mg USD 2160 In-stock
100 mg USD 3000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.

IC50 & Target

EC50: 0.43 nM (RSV)[1]

In Vitro

Presatovir is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a hit originated from a phenotypic RSV antiviral high-throughput screen. Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates with a mean EC50 value of 0.43 nM[1]. GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity[2].

In Vivo

Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy in a cotton rat model of RSV infection. 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 is observed in the high dose group. A group treated with a lower dose of Presatovir allows for a PK-PD relationship to be established to help guide future dose selections[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.8795 mL 9.3974 mL 18.7949 mL
5 mM 0.3759 mL 1.8795 mL 3.7590 mL
10 mM 0.1879 mL 0.9397 mL 1.8795 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

GS-5806 are 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 1×105 cells/mL, are infected in bulk with RSV A2 at a titer of approximately 1×104.5 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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

532.06

Formula

C₂₄H₃₀ClN₇O₃S

CAS No.

1353625-73-6

SMILES

O=C(C(C=C(Cl)C=C1)=C1NS(C)(=O)=O)N(CCCC2)[[email protected]@H]2C3=NN4C(N=C(N5CC[[email protected]](N)C5)C(C)=C4)=C3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Presatovir
Cat. No.:
HY-16727
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