GS-443902
Based on 13 publication(s) in Google Scholar
GS-443902 (GS-441524 triphosphate) 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 is the active triphosphate metabolite of Remdesivir.
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- CAS No.: 1355149-45-9
- Formule: C12H16N5O13P3
- Masse moléculaire:531.20
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Stockage:
-20°C, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GS-443902
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 Sep 18:387:114245. [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]
- bioRxiv. 2021 Jul 21:2021.07.21.453274. [Abstract]
- Research Square Preprint. 2022 May.
- Curr Res Pharmacol Drug Discov. 2021:2:100045. [Abstract]
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>200 μM
Compound: 4tp
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Inhibition of RNA polymerase 2 in human HeLa cells preincubated for 5 mins with dATP/dGTP/dTTP as substrate followed by addition of cell extract measured after 1 hr by SDS-PAGE method
Inhibition of RNA polymerase 2 in human HeLa cells preincubated for 5 mins with dATP/dGTP/dTTP as substrate followed by addition of cell extract measured after 1 hr by SDS-PAGE method
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[PMID: 28124907] |
In a continuous 72 h incubation of 1 µM Remdesivir (GS-5734), the GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; compound 4tp) 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 (compound 8a) is a triphosphates (TP) derivative[2].
GS-443902 (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[3].
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.
Chemical Information
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CAS No. 1355149-45-9
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Appearance Solid
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Masse moléculaire 531.20
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Formule C12H16N5O13P3
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Color Light yellow to yellow
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SMILES
O=P(OP(O)(O)=O)(O)OP(OC[C@@H](O1)[C@@H](O)[C@@H](O)[C@]1(C#N)C2=CC=C3N2N=CN=C3N)(O)=O
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Synonyms
GS-441524 triphosphate; Remdesivir metabolite
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, 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 Sep 18:387:114245. 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 -
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 -
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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
Solvant et solubilité
H2O : 100 mg/mL (188.25 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)
Pureté et documentation
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Fiche technique (277 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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Instruction de manipulation (2659 KB)
Références
[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]. 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]
[3]. 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]
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 | 1.8825 mL | 9.4127 mL | 18.8253 mL | 47.0633 mL |
| 5 mM | 0.3765 mL | 1.8825 mL | 3.7651 mL | 9.4127 mL | |
| 10 mM | 0.1883 mL | 0.9413 mL | 1.8825 mL | 4.7063 mL | |
| 15 mM | 0.1255 mL | 0.6275 mL | 1.2550 mL | 3.1376 mL | |
| 20 mM | 0.0941 mL | 0.4706 mL | 0.9413 mL | 2.3532 mL | |
| 25 mM | 0.0753 mL | 0.3765 mL | 0.7530 mL | 1.8825 mL | |
| 30 mM | 0.0628 mL | 0.3138 mL | 0.6275 mL | 1.5688 mL | |
| 40 mM | 0.0471 mL | 0.2353 mL | 0.4706 mL | 1.1766 mL | |
| 50 mM | 0.0377 mL | 0.1883 mL | 0.3765 mL | 0.9413 mL | |
| 60 mM | 0.0314 mL | 0.1569 mL | 0.3138 mL | 0.7844 mL | |
| 80 mM | 0.0235 mL | 0.1177 mL | 0.2353 mL | 0.5883 mL | |
| 100 mM | 0.0188 mL | 0.0941 mL | 0.1883 mL | 0.4706 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.
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