GS-5806 MedChemExpress (MCE)

Product Name	Presatovir
Synonyms	CS-2075 GS-5806 Presatovir Presatovir (GS-5806) N-(2-((S)-2-(5-((S)-3-aminopyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)piperidine-1-carbonyl)-4-chlorophenyl)methanesulfonamide N-(2-{[(2S)-2-{5-[(3S)-3-Amino-1-pyrrolidinyl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl}-1-piperidinyl]carbonyl}-4-chlorophenyl)methanesulfonamide Synonyms CS-2075 GS-5806 Presatovir Presatovir (GS-5806) N-(2-((S)-2-(5-((S)-3-aminopyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)piperidine-1-carbonyl)-4-chlorophenyl)methanesulfonamide N-(2-{[(2S)-2-{5-[(3S)-3-Amino-1-pyrrolidinyl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl}-1-piperidinyl]carbonyl}-4-chlorophenyl)methanesulfonamide Methanesulfonamide, N-[2-[[(2S)-2-[5-[(3S)-3-amino-1-pyrrolidinyl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl]-1-piperidinyl]carbonyl]-4-chlorophenyl]-
CAS	1353625-73-6
EINECS
Chemical Formula	C24H30ClN7O3S
Molecular Weight	532.06
inchi
Package	1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	Presatovir Presatovir MedChemExpress (MCE) HY-16727 1353625-73-6 GS-5806 99.91% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Presatovir Presatovir MedChemExpress (MCE) HY-16727 1353625-73-6 GS-5806 99.91% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM. 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]. 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]. 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]. EC50: 0.43 nM (RSV)[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief]
Supplier Website	https://www.medchemexpress.com/Presatovir.html
Last Update	2025-05-21 16:50:25

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