GS-621763
Based on 1 Customer Validation
GS-621763 is an orally available precursor to GS-441524 that exhibits anti-SARS-CoV-2 viral activity in mice. GS-621763 reduces viral load to undetectable levels in ferrets infected with SARS-CoV-2.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.72%
- CAS. Nr.: 2647442-13-3
- Formel: C24H31N5O7
- Molecular Weight:501.53
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| HEp-2 | CC50 |
81 μM
Compound: 13
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Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay
Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay
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[PMID: 33835812] |
| HEp-2 | EC50 |
0.26 μM
Compound: 13
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Antiviral activity against RSV A2 infected in HEp-2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by CellTiter Glo viability assay
Antiviral activity against RSV A2 infected in HEp-2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by CellTiter Glo viability assay
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[PMID: 33835812] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SARS-CoV-2 infected BALB/c mouse model[1]
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Dosage:30 mg/kg and 60 mg/kg
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Administration:Oral gavage (p.o.), twice daily for 4 days
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Result:Significantly reduced lung infectious virus levels (30 mg/kg); Further reduced ung infectious virus levels (60 mg/kg).
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Animal Model:SARS-CoV-2-infected ferret model[2]
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.), twice daily for 4 days
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Result:Significantly reduced SARS-CoV-2 shedding, with virus undetectable in nasal lavages.
Chemical Information
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CAS. Nr. 2647442-13-3
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Appearance Solid
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Molecular Weight 501.53
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Formel C24H31N5O7
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Color White to off-white
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SMILES
N#C[C@]1(C2=CC=C3N2N=CN=C3N)[C@@H]([C@@H]([C@H](O1)COC(C(C)C)=O)OC(C(C)C)=O)OC(C(C)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (199.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (4.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.98 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Schäfer A, et al. Therapeutic efficacy of an oral nucleoside analog of remdesivir against SARS-CoV-2 pathogenesis in mice. bioRxiv [Preprint]. 2021 Sep 17:2021.09.13.460111. [Content Brief]
[2]. Cox RM, et al. Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets. Nat Commun. 2021 Nov 5;12(1):6415. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9939 mL | 9.9695 mL | 19.9390 mL | 49.8475 mL |
| 5 mM | 0.3988 mL | 1.9939 mL | 3.9878 mL | 9.9695 mL | |
| 10 mM | 0.1994 mL | 0.9969 mL | 1.9939 mL | 4.9847 mL | |
| 15 mM | 0.1329 mL | 0.6646 mL | 1.3293 mL | 3.3232 mL | |
| 20 mM | 0.0997 mL | 0.4985 mL | 0.9969 mL | 2.4924 mL | |
| 25 mM | 0.0798 mL | 0.3988 mL | 0.7976 mL | 1.9939 mL | |
| 30 mM | 0.0665 mL | 0.3323 mL | 0.6646 mL | 1.6616 mL | |
| 40 mM | 0.0498 mL | 0.2492 mL | 0.4985 mL | 1.2462 mL | |
| 50 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9969 mL | |
| 60 mM | 0.0332 mL | 0.1662 mL | 0.3323 mL | 0.8308 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2492 mL | 0.6231 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4985 mL |
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