Remdesivir (GS-5734)

Catalog No.S8932 Batch:S893204

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	16 mg/mL (26.55 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 88 publications

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
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
Preclinical development of kinetin as a safe error-prone SARS-CoV-2 antiviral able to attenuate virus-induced inflammation [ Nat Commun, 2023, 14(1):199]	PubMed: 36639383
Pharmacological inhibition of TBK1/IKKε blunts immunopathology in a murine model of SARS-CoV-2 infection [ Nat Commun, 2023, 14(1):5666]	PubMed: 37723181
Innate immune pathway modulator screen identifies STING pathway activation as a strategy to inhibit multiple families of arbo and respiratory viruses [ Cell Rep Med, 2023, 4(5):101024]	PubMed: 37119814
Pharmacological inhibition of TBK1/IKKε blunts immunopathology in a murine model of SARS-CoV-2 infection [ Nat Commun, 2023, 14(1):5666]	PubMed: 37723181
Ovatodiolide inhibits SARS-CoV-2 replication and ameliorates pulmonary fibrosis through suppression of the TGF-β/TβRs signaling pathway [ Biomed Pharmacother, 2023, 161:114481]	PubMed: 36906971
Activation of the urotensin-II receptor by remdesivir induces cardiomyocyte dysfunction [ Commun Biol, 2023, 6(1):511]	PubMed: 37173432
Heat shock protein 90 facilitates SARS-CoV-2 structural protein-mediated virion assembly and promotes virus-induced pyroptosis [ J Biol Chem, 2023, 299(5):104668]	PubMed: 37011862

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SHIPPING AND STORAGE
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