Presatovir
Based on 6 publication(s) in Google Scholar
Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.26%
- CAS. Nr.: 1353625-73-6
- Formel: C24H30ClN7O3S
- Molecular Weight:532.06
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Presatovir
More
Biologische Aktivität
EC50: 0.43 nM (RSV)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEp-2 | CC50 |
>20 μM
Compound: 3, GS-5806
|
Cytotoxicity against human Hep2 cells after 4 days by cell-Titer Glo assay
Cytotoxicity against human Hep2 cells after 4 days by cell-Titer Glo assay
|
[PMID: 25574686] |
| HEp-2 | EC50 |
0.1 nM
Compound: 1; GS-5806
|
Inhibition of Human respiratory syncytial virus A2 Fusion protein expressed in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by Celltiter-Glo viability assay
Inhibition of Human respiratory syncytial virus A2 Fusion protein expressed in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by Celltiter-Glo viability assay
|
[PMID: 32550994] |
| HEp-2 | EC50 |
0.37 nM
Compound: 3, GS-5806
|
Antiviral activity against Respiratory syncytial virus A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathogenicity after 4 days by cell-Titer Glo assay
Antiviral activity against Respiratory syncytial virus A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathogenicity after 4 days by cell-Titer Glo assay
|
[PMID: 25574686] |
| HEp-2 | EC50 |
1193 nM
Compound: 1; GS-5806
|
Inhibition of Human respiratory syncytial virus Fusion protein D486N mutant expressed in Hep2 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 hrs followed by replacement of fresh medium containing compounds and measured afte
Inhibition of Human respiratory syncytial virus Fusion protein D486N mutant expressed in Hep2 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 hrs followed by replacement of fresh medium containing compounds and measured afte
|
[PMID: 32550994] |
| MT4 | CC50 |
>20 μM
Compound: 3, GS-5806
|
Cytotoxicity against human MT4 cells
Cytotoxicity against human MT4 cells
|
[PMID: 25574686] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 1353625-73-6
-
Appearance Solid
-
Molecular Weight 532.06
-
Formel C24H30ClN7O3S
-
Color Off-white to light yellow
-
SMILES
O=C(C(C=C(Cl)C=C1)=C1NS(C)(=O)=O)N(CCCC2)[C@@H]2C3=NN4C(N=C(N5CC[C@H](N)C5)C(C)=C4)=C3
-
Synonyms
GS-5806
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
J Enzyme Inhib Med Chem
The mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus. [Abstract]2022 Dec;37(1):2598-2604. PMID: 36131622 -
J Virol
Molecular mechanism of resistance to lonafarnib conferred by mutations in the cysteine-rich region of respiratory syncytial virus fusion glycoprotein and discovery of a lonafarnib-derived antiviral PROTAC. [Abstract]2025 Dec 9:e0148725. PMID: 41364004 -
J Virol
Mechanism of Cross-Resistance to Fusion Inhibitors Conferred by the K394R Mutation in Respiratory Syncytial Virus Fusion Protein. [Abstract]2021 Sep 27;95(20):e0120521. PMID: 34379500 -
J Antimicrob Chemother
Differential antiviral activities of respiratory syncytial virus (RSV) inhibitors in human airway epithelium. [Abstract]2018 Jul 1;73(7):1823-1829. PMID: 29596680 -
Npj Viruses
STAT1 signaling controls cholesterol metabolism in epithelial cells and RSV-induced syncytia formation. [Abstract]2026 Feb 16;4(1):10. PMID: 41699197 -
Lösungsmittel & Löslichkeit
DMSO : 6 mg/mL (11.28 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 0.6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 0.6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8795 mL | 9.3974 mL | 18.7949 mL | 46.9872 mL |
| 5 mM | 0.3759 mL | 1.8795 mL | 3.7590 mL | 9.3974 mL | |
| 10 mM | 0.1879 mL | 0.9397 mL | 1.8795 mL | 4.6987 mL |
Presatovir Related Classifications
HY-16727 Related Classifications
Powered by Bioz