Remdesivir (GS-5734)

Catalog No.S8932

For research use only.

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

CAS No. 1809249-37-3

Selleck's Remdesivir (GS-5734) has been cited by 61 publications

Purity & Quality Control

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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 M1\rWmFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= MlrUOEBl[Xm| NWjXWmNkTUN3MDC9JFAvODF3IN88US=> M2HRelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUK0PVA4Lz5{OEGyOFkxPzxxYU6=
TERT-immortalized HMVEC NXnqSGJQSW62aY\pdoFtKGGldHn2bZR6KGG|c3H5 MY[zJJRwKDRiZHH5dy=> MVXFR|UxKD1iMD6wOVMh|ryP NUjlUJlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
HuH7 M2\TbGFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= NGHT[ZE{KGSjeYO= M{fJcmVEPTBiPTCwMlA2PyEQvF2= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
HuH7 M1HLUGFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= MmHlN{Bl[Xm| MkHXSWM2OCB;IECuNFch|ryP MmDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5OUK3OlMoRjJ6N{myO|Y{RC:jPh?=
macrophages MnfORY51cX[rcnHsJIFkfGm4aYT5JIF{e2G7 M1jWdlQ5KGh? NGPkVY5GSzVyIE2gNE4xQDZizszN MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
macrophages M{\zUGFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= NHj2NI41QCCq M3LMPGVEPTBiPTCwMlA5PiEQvF2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2N{c,Ojh5OUK3OlM9N2F-
HeLa MYLBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? M1fhSVQ5KGh? M3KwS2VEPTBiPTCwMlEh|ryP NXrVVHJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
HeLa NIr4T3lCdnSrdnnyZYwh[WO2aY\peJkh[XO|YYm= NV;JVIZGPDhiaB?= MkjDSWM2OCB;IECuNVQh|ryP NFfWZlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3Oyd-Mki3PVI4PjN:L3G+
MT4 NI\PW5pEgXSxdH;4bYNqfHliYYPzZZk> MoDrOEB1dyB3IHThfZM> M2LDcGNEPTBiPTCxMlch|ryP NV\XZoJ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
Hep2 NWjBcI05S3m2b4TvfIlkcXS7IHHzd4F6 Mn;OOEB1dyB3IHThfZM> MmPxR2M2OCB;IE[uNUDPxE1? M2KzfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUK0PVA4Lz5{OEGyOFkxPzxxYU6=
HuH7 M{XERWN6fG:2b4jpZ4l1gSCjc4PhfS=> MWizJIRigXN? M2riWmNEPTBiPTCzOkDPxE1? NXzvXZhyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
Assay
Methods Test Index PMID
Western blot delayed chain termination of RNA synthesis ; tGFP-BlaR / Actin ; ACE2 / Actin ; VP0 / VP2 30987343 33835389 32793908 32595613
Growth inhibition assay Cell viability ; Cell viability ; Cell viability 33835389 33186749 32595613
Pharmacokinetics plasma concentration ; plasma concentration 32589775 33782830
Immunofluorescence MERS-CoV S Protein ; viral S protein and E-caherin ; SARS-CoV-2 / E‐cadherin / VE‐cadherin ; SARS-CoV-2 ; viral dsRNA replication intermediates 33376043 33186749 33173719 32869028 32595613
Viral loads and virus titers SARS-CoV-2 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 (from reference)

Animal Research:

[1]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 602.58
Formula

C27H35N6O8P

CAS No. 1809249-37-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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