Remdesivir (GS-5734)

For research use only.

Catalog No.S8932

35 publications

Remdesivir (GS-5734) Chemical Structure

CAS No. 1809249-37-3

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.

Selleck's Remdesivir (GS-5734) has been cited by 35 publications

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep2 NGq4bmlCdnSrdnnyZYwh[WO2aY\peJkh[XO|YYm= MVK0JIRigXN? M3XPb2VEPTBiPTCwMlAyPSEQvF2= MlnVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzMkS5NFcoRjJ6MUK0PVA4RC:jPh?=
TERT-immortalized HMVEC MkPuRY51cX[rcnHsJIFkfGm4aYT5JIF{e2G7 M{\WU|MhfG9iNDDkZZl{ NYHXRVZMTUN3MDC9JFAvODV|IN88US=> M{fHVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUK0PVA4Lz5{OEGyOFkxPzxxYU6=
HuH7 MkjyRY51cX[rcnHsJIFkfGm4aYT5JIF{e2G7 NUH0XFF[OyCmYYnz MWLFR|UxKD1iMD6wOVch|ryP NYHOSohpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
HuH7 MVjBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? M4DmVVMh\GG7cx?= NFTHcG1GSzVyIE2gNE4xPyEQvF2= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2N{c,Ojh5OUK3OlM9N2F-
macrophages NWX1eWgxSW62aY\pdoFtKGGldHn2bZR6KGG|c3H5 NYDk[5BMPDhiaB?= MlLXSWM2OCB;IECuNFg3KM7:TR?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
macrophages MV;BcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? MmrwOFghcA>? Mn63SWM2OCB;IECuNFg3KM7:TR?= NVLtTIhlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjNpPkK4O|kzPzZ|PD;hQi=>
HeLa MYDBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? MYO0PEBp MXvFR|UxKD1iMD6xJO69VQ>? NHv0cHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGyOFkxPyd-MkixNlQ6ODd:L3G+
HeLa MVjBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? MlvMOFghcA>? NYrOXlBGTUN3MDC9JFAvOTRizszN NYjJWZBlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjNpPkK4O|kzPzZ|PD;hQi=>
MT4 M4LxcWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1v3SFQhfG9iNTDkZZl{ NGTES4ZESzVyIE2gNU44KM7:TR?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
Hep2 NIXJTlREgXSxdH;4bYNqfHliYYPzZZk> M1rsdVQhfG9iNTDkZZl{ M2j4d2NEPTBiPTC2MlEh|ryP MnPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzMkS5NFcoRjJ6MUK0PVA4RC:jPh?=
HuH7 NILUcmNEgXSxdH;4bYNqfHliYYPzZZk> NFi3dYg{KGSjeYO= M{\DcWNEPTBiPTCzOkDPxE1? NEiyUVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGyOFkxPyd-MkixNlQ6ODd:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
delayed chain termination of RNA synthesis; 

PubMed: 30987343     


Effective delayed chain termination of RNA synthesis by remdesivir. (A) Remdesivir-MP-dependent delayed chain termination of RNA synthesis was studied with purified EBOV RdRp. RNA synthesis was monitored in the presence of [α-32P]GTP, CTP, and ATP or remdesivir-TP, supplemented with increasing concentrations of UTP for incorporation at position i+6, representing a 12-nt RNA product labeled 12.

tGFP-BlaR / Actin; 

PubMed: 33835389     


Thirty-six hours post-transfection, Western blot for tGFP-BlaR expression is carried out with remdesivir treated cells.

ACE2 / Actin; 

PubMed: 32793908     


(C) Remdesivir alone increased ACE2 protein expression. H1299 human NSCLC cells, MSTO-211H human mesothelioma cells, and Calu-3 human NSCLC type II alveolar cells were treated with remdesivir and VS-6766 for 48 hours. ACE2 was probed with Abnova PAB13444 antibody, and β-Actin was probed with Sigma A5441 antibody as a loading control.

VP0 / VP2; 

PubMed: 32595613     


(C) Western blot of EV71 VP2 protein expression in HeLa cells. HeLa cells were infected with EV71 (MOI = 0.5). After adsorption, the cells were treated with the indicated concentrations of remdesivir and collected at 24 hpi. Then, the proteins were resolved by SDS-PAGE and western blotting.

30987343 33835389 32793908 32595613
Growth inhibition assay
Cell viability; 

PubMed: 33835389     


293 T cells are transfected with SARS-CoV-2-GFP replicon, remdesivir is added to culture media 10 h post transfection or just before transfection respectively, the green fluorescence intensity is determined thirty-six hours post-transfection, and dose responsive curves are drawn and EC50 value of remdesivir (B) was calculated by four-parameter nonlinear regression respectively.

Cell viability; 

PubMed: 33186749     


Remdesivir inhibits SARS-CoV-2 infection of PSC-HIOs. (B) Effect of remdesivir on metabolic activity of Caco-2 cells was assessed by CellTiter-Glo assay. Shown are technical triplicates from one representative experiment. Error bars represent SEM.

Cell viability; 

PubMed: 32595613     


(B) Cell viability after culture with different doses of remdesivir at 24 hpi assessed using a CCK8 assay (mean ± SD, n = 6).

33835389 33186749 32595613
Pharmacokinetics
plasma concentration; 

PubMed: 32589775     


Plasma concentration‐vs‐time profiles following RDV single‐dose administration; mean (±SD) values are plotted. LLOQ, lower limit of quantification; RDV, remdesivir.

plasma concentration; 

PubMed: 33782830     


Mean (standard deviation) of remdesivir (RDV) plasma concentration vs time by dose following 30-min intravenous infusion(s) of a single 200-mg dose or multiple 100-mg remdesivir doses in healthy subjects.

32589775 33782830
Immunofluorescence
MERS-CoV S Protein; 

PubMed: 33376043     


Dose-dependent inhibition of MERS-CoV infection by lycorine. (B) The confocal microscope images showed cell nuclei (red) and MERS-CoV spike (S) protein (green) at the indicated lycorine concentration or 8.3 μM remdesivir (RDV) after MERS-CoV infection. Scale bar = 100 μM.

viral S protein and E-caherin; 

PubMed: 33186749     


(C) PSC-HIOs were infected with SARS-CoV-2 and treated with indicated concentrations of remdesivir. Two days later, infection was analyzed by viral S protein and E-caherin (Ecad, green) staining. Nuclei are stained with DAPI in blue. Scale bar = 50 μM. Images are representative for at least 3 independent experiments.

SARS-CoV-2 / E‐cadherin / VE‐cadherin; 

PubMed: 33173719     


Evaluation of potential antiviral efficacy of remdesivir on the chip system. B) Confocal immunofluorescent microscopy images of epithelium (E‐cadherin) and endothelium (VE‐cadherin) of alveolus chip treated without or with 1 × 10−6 m remdesivir at day 2 post‐infection.

SARS-CoV-2; 

PubMed: 32869028     


Antiviral SARS-CoV-2 activity and cytotoxicity of PF-00835231, and remdesivir in A549+ACE2 cells. f. Representative images of SARS-CoV-2 USA-WA1/2020 syncytia formation at 48 hpi in A549+ACE2 cells under treatment with 0.33 μM PF-00835231, or remdesivir.

viral dsRNA replication intermediates; 

PubMed: 32595613     


(D) Fluorescence microscopy examination of EV71-infected HeLa cells treated with different amounts of remdesivir (24 hpi). The dsRNA-specific antibody J2 (red) was used for staining viral dsRNA replication intermediates, and nuclei were labeled with Hoechst 33258 (blue). Bar = 100 μm.

33376043 33186749 33173719 32869028 32595613
Viral loads and virus titers
SARS-CoV-2; 

PubMed: 32516797     


Viral loads and virus titers in swabs collected from rhesus macaques infected with SARS-CoV-2 and treated with remdesivir. Panel A shows viral loads and Panel B shows infectious virus titers in nose, throat and rectal swabs collected daily from animals treated with remdesivir (n=6) or vehicle solution (n=6). Statistical analysis was performed using a 2-way ANOVA with Sidak’s multiple comparisons test.

32516797
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]

Protocol

Animal Research:

[1]

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  • Animal Models: Rhesus monkeys (Macaca mulatta)
  • Dosages: 3 mg / kg, 10 mg / kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (165.95 mM)
Water Insoluble
Ethanol ''''16 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 602.58
Formula

C27H35N6O8P

CAS No. 1809249-37-3
Storage powder
in solvent
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02818582 Completed Drug: GS-5734|Other: Placebo Comparator Ebola National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) July 1 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID