1353625-73-6
1353625-73-6 structure
- Name: Presatovir
- Chemical Name: Presatovir
- CAS Number: 1353625-73-6
- Molecular Formula: C24H30ClN7O3S
- Molecular Weight: 532.058
- Catalog: Signaling Pathways Anti-infection RSV
- Create Date: 2018-10-17 12:36:58
- Modify Date: 2024-01-15 11:56:44
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Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.
| Name | Presatovir |
|---|---|
| Synonyms |
UNII-9628AJ27JA
GS-5806 presatovir 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]- 9628AJ27JA |
| Description | Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM. |
|---|---|
| Related Catalog | |
| 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]. |
| Cell Assay | 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]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C24H30ClN7O3S |
| Molecular Weight | 532.058 |
| Exact Mass | 531.181946 |
| LogP | 1.79 |
| Index of Refraction | 1.735 |
| Storage condition | 2-8℃ |