1. Anti-infection
  2. RSV

Presatovir (Synonyms: GS-5806)

Cat. No.: HY-16727 Purity: 98.34%
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
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 2160 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 3000 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Featured Recommendations

  • 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
Solvent & Solubility
In Vitro: 

H2O : < 0.1 mg/mL (insoluble)

DMSO : 6 mg/mL (11.28 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution

References
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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Presatovir
Cat. No.:
HY-16727
Quantity:

Presatovir

Cat. No.: HY-16727