Remdesivir (GS-5734) Antiviral Agent

Cat.No.S8932

Remdesivir (GS-5734) is a monophosphoramidate prodrug of an adenosine analog and an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.
Remdesivir (GS-5734) Antiviral inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 602.58

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep2 Antiviral activity assay 4 days EC50 = 0.015 μM 28124907
TERT-immortalized HMVEC Antiviral activity assay 3 to 4 days EC50 = 0.053 μM 28124907
HuH7 Antiviral activity assay 3 days EC50 = 0.057 μM 28124907
HuH7 Antiviral activity assay 3 days EC50 = 0.07 μM 28792763
macrophages Antiviral activity assay 48 h EC50 = 0.086 μM 28124907
macrophages Antiviral activity assay 48 h EC50 = 0.086 μM 28792763
HeLa Antiviral activity assay 48 h EC50 = 0.1 μM 28124907
HeLa Antiviral activity assay 48 h EC50 = 0.14 μM 28792763
MT4 Cytotoxicity assay 4 to 5 days CC50 = 1.7 μM 28124907
Hep2 Cytotoxicity assay 4 to 5 days CC50 = 6.1 μM 28124907
HuH7 Cytotoxicity assay 3 days CC50 = 36 μM 28124907
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 602.58 Formula

C27H35N6O8P

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1809249-37-3 -- Storage of Stock Solutions

Synonyms N/A Smiles CCC(CC)COC(=O)C(C)NP(=O)(OCC1C(C(C(O1)(C#N)C2=CC=C3N2N=CN=C3N)O)O)OC4=CC=CC=C4

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (165.95 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro

Remdesivir (GS-5734) exhibits antiviral activity against multiple variants of EBOV in cell-based assays (EC50=0.06-0.14 μM) and broad-spectrum antiviral activity in vitro against other pathogenic RNA viruses. [1]

This compound acts as a broad-spectrum therapeutic to protect against CoVs with EC50 of 0.03 μM for murine hepatitis virus in delayed brain tumor cells and 0.074 μM for SARS-CoV and MERS-CoV in HAE cells.[2]

In vivo

Regardless of the time of initiation, treatment with Remdesivir (GS-5734) at 3 mg/kg confers improved survival. All animals in which a 10 mg/kg regimen is initiated 3 days after virus exposure survive to the end of the in-life phase. However, the antiviral effects are consistently greater in animals administered repeated 10 mg/kg doses. The 10 mg/kg D3 (administered beginning 3 days after virus exposure) regimen is associated with amelioration of EVD-related clinical disease signs and markers of coagulopathy and end organ pathophysiology.[1]

References

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