Home Microbiology Antiviral inhibitor - DNA/RNA Synthesis inhibitor - COVID-19 inhibitor Remdesivir (GS-5734) For research use only.

Remdesivir (GS-5734)

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

Remdesivir (GS-5734) Chemical Structure

Remdesivir (GS-5734) Chemical Structure

CAS: 1809249-37-3

Selleck's Remdesivir (GS-5734) has been cited by 84 publications

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Cell Data

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

Biological Activity

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

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]

GS-5734 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]
Cell Research Cell lines HeLa cells
Concentrations 0.14 uM
Incubation Time 72 h
Method

Cells were treated with various concentrations of GS-5734.
Experimental Result Images Methods Biomarkers Images PMID
Western blot VP0 / VP2 ACE2 / Actin tGFP-BlaR / Actin delayed chain termination of RNA synthesis 32595613
Growth inhibition assay Cell viability Cell viability Cell viability 32595613
Immunofluorescence viral dsRNA replication intermediates SARS-CoV-2 SARS-CoV-2 / E‐cadherin / VE‐cadherin viral S protein and E-caherin MERS-CoV S Protein 32595613
Pharmacokinetics plasma concentration plasma concentration 33782830
Viral loads and virus titers SARS-CoV-2 32516797
In Vivo
In vivo

Regardless of the time of initiation, GS-5734 treatment confers improved survival when administered by 3 mg/kg GS-5734. All animals in which 10 mg/kg GS-5734 treatments 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 GS-5734 doses. The 10 mg/kg D3 (administered beginning 3 days after virus exposure) GS-5734 regimen is associated with amelioration of EVD-related clinical disease signs and markers of coagulopathy and end organ pathophysiology.[1]
Animal Research Animal Models Rhesus monkeys (Macaca mulatta)
Dosages 3 mg / kg, 10 mg / kg
Administration IV

Chemical lnformation & Solubility

Molecular Weight 602.58 Formula

C27H35N6O8P
CAS No. 1809249-37-3 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (165.95 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble


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In vivo
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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.

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