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GS-443902 trisodium

Name: GS-443902 trisodium
Brand: TargetMol
SKU: T38761
Rating: 4.5 (1 reviews)

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Catalog No. T38761Cas No. 1355050-21-3

Alias Remdesivirmetabolitetrisodium, GS-441524triphosphatetrisodium

GS-443902 trisodium (GS-441524 triphosphate trisodium), the active triphosphate metabolite of Remdesivir (GS-5734), serves as a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), displaying inhibitory concentrations (IC50) of 1.1 μM for RSV RdRp and 5 μM for HCV RdRp.

GS-443902 trisodium

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Catalog No. T38761Alias Remdesivirmetabolitetrisodium, GS-441524triphosphatetrisodiumCas No. 1355050-21-3

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	Inquiry	10-14 weeks	10-14 weeks
5 mg	Inquiry	10-14 weeks	10-14 weeks
10 mg	Inquiry	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	GS-443902 trisodium (GS-441524 triphosphate trisodium), the active triphosphate metabolite of Remdesivir (GS-5734), serves as a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), displaying inhibitory concentrations (IC50) of 1.1 μM for RSV RdRp and 5 μM for HCV RdRp.
Targets&IC50	HCV RdRp:5 µM (IC50), RdRp (RSV):1.1 µM (IC50)
In vitro	During a 72-hour incubation with 1 μM Remdesivir (GS-5734), levels of its metabolite, GS-443902 trisodium (GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium), were monitored at intervals of 2, 24, 48, and 72 hours, showing peak concentrations (C max) of 300, 110, and 90 pmol/million cells in macrophages, HMVEC, and HeLa cell lines, respectively[1]. GS-443902 trisodium (compound 8a), a triphosphate (TP) derivative[2], impairs RSV RdRp-catalyzed RNA synthesis through integration into the nascent viral RNA, resulting in its premature termination. It is effectively transformed within cells to GS-443902 sodium, which selectively disrupts Ebola virus (EBOV) replication by targeting and inhibiting the viral RNA-dependent RNA polymerase (RdRp), thus blocking viral RNA synthesis[3].
In vivo	Remdesivir (GS-5734; 10?mg?kg; i.v.) rapidly distributes into peripheral blood mononuclear cells (PBMCs), and efficient conversion to GS-443902 trisodium (Remdesivir metabolite trisodium; NTP) is apparent within 2?h of dose administration in rhesus monkeys. In PBMCs, GS-443902 trisodium 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].
Synonyms	Remdesivirmetabolitetrisodium, GS-441524triphosphatetrisodium

Chemical Properties

Formula	C₁₂H₁₆N₅O₁₃P₃.xNa
Cas No.	1355050-21-3
Smiles	C(#N)[C@]1(O[C@H](COP(OP(OP(=O)(O)O)(=O)O)(=O)O)[C@@H](O)[C@H]1O)C=2N3C(=CC2)C(N)=NC=N3.[Na]
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc