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Presatovir

Catalog No. TQ0085 CAS 1353625-73-6

Synonyms: GS-5806

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Presatovir, CAS 1353625-73-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 263.00
10 mg	In stock	$ 428.00
25 mg	In stock	$ 716.00
50 mg	In stock	$ 987.00
100 mg	In stock	$ 1,370.00
500 mg	In stock	$ 2,730.00

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Purity: 99.38%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Presatovir (GS-5806) (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor (mean EC50: 0.43 nM).
Targets&IC50	RSV:0.43 nM (EC50)
In vitro	Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates (mean EC50: 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	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 [1].
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 [1].

Synonyms	GS-5806
Molecular Weight	532.06
Formula	C24H30ClN7O3S
CAS No.	1353625-73-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (9.4 mM), Sonication and heating are recommended.

H2O: Insoluble

References and Literature

1. Mackman RL, et al. Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study. J Med Chem. 2015 Feb 26;58(4):1630-1643. 2. Samuel D, et al. GS-5806 inhibits pre- to postfusion conformational changes of the respiratory syncytial virus fusion protein. Antimicrob Agents Chemother. 2015 Nov;59(11):7109-12.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Clinical Compound Library Pediatric Drug Library Orally Active Compound Library NO PAINS Compound Library Anti-Infection Compound Library Bioactive Compounds Library Max Anti-Viral Compound Library Bioactive Compound Library

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Related compounds with same targets

Amentoflavone Ziresovir RSV604 JNJ-8003 Lumicitabine KIN101 Ac-CoA Synthase Inhibitor1 GS-443902

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Presatovir 1353625-73-6 Microbiology/Virology RSV inhibit GS-5806 Inhibitor Respiratory syncytial virus GS 5806 GS5806 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.