Remdesivir (GS-5734)

Catalog No.S8932 Batch:S893202

Technical Data

Formula	C₂₇H₃₅N₆O₈P
Molecular Weight	602.58	CAS No.	1809249-37-3
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (165.95 mM)
		Ethanol	25 mg/mL (41.48 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]
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]

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]

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)

Cell Assay:^{^[1]}	Cell lines HeLa cells Concentrations 0.14 uM Incubation Time 72 h Method Cells were treated with various concentrations of GS-5734.
Animal Study:^{^[1]}	Animal Models Rhesus monkeys (Macaca mulatta) Dosages 3 mg / kg, 10 mg / kg Administration IV

References

Selleck's Remdesivir (GS-5734) has been cited by 98 publications

The host-targeted antiviral drug Zapnometinib exhibits a high barrier to the development of SARS-CoV-2 resistance [ Antiviral Res, 2024, 225:105840]	PubMed: 38438015
Unveiling the Antiviral Properties of Panduratin A through SARS-CoV-2 Infection Modeling in Cardiomyocytes [ Int J Mol Sci, 2024, 25(3)1427]	PubMed: 38338708
Unveiling the Antiviral Properties of Panduratin A through SARS-CoV-2 Infection Modeling in Cardiomyocytes [ Int J Mol Sci, 2024, 24;25(3):1427.]	PubMed: 38338708
Development of a Měnglà virus minigenome and comparison of its polymerase complexes with those of other filoviruses [ Virol Sin, 2024, 39(3):459-468]	PubMed: 38782261
The PKA-CREB1 axis regulates coronavirus proliferation by viral helicase nsp13 association [ J Virol, 2024, 98(4):e0156523]	PubMed: 38445884
Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Biological and Pharmacological Profiling [ Viruses, 2024, 16(7)1158]	PubMed: 39066320
A high-throughput response to the SARS-CoV-2 pandemic [ SLAS Discov, 2024, 29(5):100160]	PubMed: 38761981
Multiple pathways for SARS-CoV-2 resistance to nirmatrelvir [ Nature, 2023, 613(7944):558-564]	PubMed: 36351451
Multiple pathways for SARS-CoV-2 resistance to nirmatrelvir [ Nature, 2023, 613(7944):558-564]	PubMed: 36351451
A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry [ Cell, 2023, 186(4):850-863.e16]	PubMed: 36803605

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SHIPPING AND STORAGE
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