GS-443902 trisodium
Based on 13 publication(s) in Google Scholar
GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.94%
- No. CAS: 1355050-21-3
- Fòrmula: C12H13N5Na3O13P3
- Peso molecular:597.15
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Almacenamiento:Shipping with dry ice
-80°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GS-443902 trisodium
More- Cell. 2022 Nov 10;185(23):4347-4360.e17. [Abstract]
- Nat Commun. 2021 Oct 4;12(1):5811. [Abstract]
- Acta Pharm Sin B. 2021 Jun;11(6):1607-1616. [Abstract]
- J Control Release. 2025 Nov 10:387:114245. [Abstract]
- EMBO J. 2025 Jan;44(2):563-586. [Abstract]
- J Med Chem. 2025 Jun 26;68(12):12414-12433. [Abstract]
- J Med Chem. 2024 May 9;67(9):7470-7486. [Abstract]
- Int J Mol Sci. 2022 Jul 27;23(15):8302. [Abstract]
- Chem Biol Interact. 2021 Jul 1:343:109480. [Abstract]
- Sci Rep. 2022 Nov 2;12(1):18506. [Abstract]
- Research Square Preprint. 2022 May.
- Curr Res Pharmacol Drug Discov. 2021:2:100045. [Abstract]
- bioRxiv. 2021 Jul 21:2021.07.21.453274. [Abstract]
Ver todos los productos específicos de isoformas DNA/RNA Synthesis
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Actividad biológica
Descripciòn
IC50 & Target
In Vitro
In a continuous 72 h incubation of 1 μM Remdesivir (GS-5734), the GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium) level is measured at 2, 24, 48 and 72 h, and reaches a Cmax of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cells lines respectively[1].
GS-443902 trisodium (compound 8a) is a triphosphates (TP) derivative[2].
GS-443902 trisodium (NTP; 0.01, 0.1, 1, 10, 100 μM) inhibits RSV RdRp-catalysed RNA synthesis by incorporating into the nascent viral RNA transcript and causing its premature termination. GS-5734 selectively inhibits EBOV replication by targeting its RdRp and inhibiting viral RNA synthesis following efficient intracellular conversion to GS-443902 sodium[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1355050-21-3
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Appearance Solid
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Peso molecular 597.15
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Fòrmula C12H13N5Na3O13P3
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Color White to light yellow
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SMILES
O=P(OP(O)(O[Na])=O)(O[Na])OP(OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@]1(C#N)C2=CC=C3N2N=CN=C3N)(O[Na])=O
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Synonyms
GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium
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Envío
Shipping with dry ice.
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Almacenamiento
-80°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (13)
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Journal Impact Factor
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Most Recent
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Cell
A mechanism for SARS-CoV-2 RNA capping and its inhibition by nucleotide analog inhibitors. [Abstract]2022 Nov 10;185(23):4347-4360.e17. PMID: 36335936 -
Nat Commun
2021 Oct 4;12(1):5811. PMID: 34608151 -
Acta Pharm Sin B
Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment. [Abstract]2021 Jun;11(6):1607-1616. PMID: 34221871 -
J Control Release
A general nanoplatform for nucleotide drug delivery: From molecular binding to antiviral therapy. [Abstract]2025 Nov 10:387:114245. PMID: 40975176 -
EMBO J
2025 Jan;44(2):563-586. PMID: 39739115 -
J Med Chem
Identification of 4'-Thiouridine as an Orally Available Antiviral Agent Targeting Both RdRp and NiRAN Functions of SARS-CoV-2 Nsp12. [Abstract]2025 Jun 26;68(12):12414-12433. PMID: 40512093 -
J Med Chem
Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung. [Abstract]2024 May 9;67(9):7470-7486. PMID: 38690769 -
Int J Mol Sci
A Systematic Study on the Optimal Nucleotide Analogue Concentration and Rate Limiting Nucleotide of the SARS-CoV-2 RNA-Dependent RNA Polymerase. [Abstract]2022 Jul 27;23(15):8302. PMID: 35955442 -
Chem Biol Interact
2021 Jul 1:343:109480. PMID: 33887223 -
Sci Rep
Discovery of SARS-CoV-2 antiviral synergy between remdesivir and approved drugs in human lung cells. [Abstract]2022 Nov 2;12(1):18506. PMID: 36323770 -
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Curr Res Pharmacol Drug Discov
Comparison of anti-SARS-CoV-2 activity and intracellular metabolism of remdesivir and its parent nucleoside. [Abstract]2021:2:100045. PMID: 34870151 -
bioRxiv
Combination of Antiviral Drugs to Inhibit SARS-CoV-2 Polymerase and Exonuclease as Potential COVID-19 Therapeutics. [Abstract]2021 Jul 21:2021.07.21.453274. PMID: 34312622
Solvente y solubilidad
In Vitro:
H2O : 33.33 mg/mL (55.82 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (83.73 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (280 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Siegel D, et al. Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses. Med Chem. 2017 Mar 9;60(5):1648-1661. [Content Brief]
[2]. Warren TK, et al. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature. 2016 Mar 17;531(7594):381-5. [Content Brief]
[3]. Cho A, et al. Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2705-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.6746 mL | 8.3731 mL | 16.7462 mL | 41.8655 mL |
| 5 mM | 0.3349 mL | 1.6746 mL | 3.3492 mL | 8.3731 mL | |
| 10 mM | 0.1675 mL | 0.8373 mL | 1.6746 mL | 4.1866 mL | |
| 15 mM | 0.1116 mL | 0.5582 mL | 1.1164 mL | 2.7910 mL | |
| 20 mM | 0.0837 mL | 0.4187 mL | 0.8373 mL | 2.0933 mL | |
| 25 mM | 0.0670 mL | 0.3349 mL | 0.6698 mL | 1.6746 mL | |
| 30 mM | 0.0558 mL | 0.2791 mL | 0.5582 mL | 1.3955 mL | |
| 40 mM | 0.0419 mL | 0.2093 mL | 0.4187 mL | 1.0466 mL | |
| 50 mM | 0.0335 mL | 0.1675 mL | 0.3349 mL | 0.8373 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
GS-443902 trisodium Related Classifications
HY-126303C Related Classifications
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Keywords
- GS-443902 trisodium
- 1355050-21-3
- GS-441524 triphosphate trisodium
- Remdesivir metabolite trisodium
- DNA/RNA Synthesis
- SARS-CoV
- RSV
- HCV
- Drug Metabolite
- SARS coronavirus
- Respiratory syncytial virus
- Hepatitis C virus
- triphosphate
- metabolite
- Remdesivir
- GS-5734
- RNA-dependent
- RNA-polymerases
- RdRp
- TP
- GS-441524
- Inhibitor
- inhibitor
- inhibit