Art. -Nr.: HY-126303

GS-443902

(Synonyms: GS-441524 triphosphate; Remdesivir metabolite)

13 Cited Publications

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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. Nr.: 1355149-45-9
Formel: C₁₂H₁₆N₅O₁₃P₃
Molecular Weight:531.20

Speicherung:

-20°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

GS-443902 Chemical Structure

CAS. Nr.: 1355149-45-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1.1 µM (RSV RdRp) and 5 µM (HCV RdRp)^[1]^[2]

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	>200 μM Compound: 4tp	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	[PMID: 28124907]

In Vitro

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 C_max 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.

In Vivo

Remdesivir (GS-5734; 10 mg kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 (GS-441524 triphosphate; Remdesivir metabolite; NTP) is apparent within 2 h of dose administration in rhesus monkeys. In PBMCs, GS-443902 represents the predominant metabolite and is persistent with a t_1/2 of 14 h and levels required for >50% virus inhibition for 24 hours^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1355149-45-9
Appearance Solid
Molecular Weight 531.20
Formel C₁₂H₁₆N₅O₁₃P₃
Color Light yellow to yellow
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
Synonyms

GS-441524 triphosphate; Remdesivir metabolite
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (13)

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Journal Impact Factor

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

Programmable nano-reactors for stochastic sensing. [Abstract]

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

Structure of the Nipah virus polymerase complex. [Abstract]

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

Potent toxic effects of Taroxaz-104 on the replication of SARS-CoV-2 particles. [Abstract]

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
Research Square Preprint

2022 May.
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

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 100 mg/mL (188.25 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8825 mL

9.4127 mL

18.8253 mL

5 mM

0.3765 mL

1.8825 mL

3.7651 mL

10 mM

0.1883 mL

0.9413 mL

1.8825 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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.

GS-443902

13 Cited Publications

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GS-443902

Publications Citing Use of MedChemExpress (MCE) GS-443902

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GS-443902 Related Classifications

HY-126303 Related Classifications