Anti-infection inhibitor
Remdesivir, 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) 5 mg
£555.00
Chemical name: L-Alanine, N-[(S)-hydroxyphenoxyphosphinyl]-, 2-ethylbutyl ester, 6-ester with 2-C-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-D-altrononitrile
Formula: C27H35N6O8P
Molecular weight: 602.58
Purity: 99.31 %
Size: 5 mg
Storage: 3 years -20°C powder, 2 years -80°C in solvent
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]
Animal research (only for reference)
Animal Models: Rhesus monkeys (Macaca mulatta)
Formulation: 12% sulfobutylether-β-cyclodextrin (SBE-β-CD), pH adjusted to 3.0 using HCl
Dosages: 3 mg / kg, 10 mg / kg
Administration: IV
References:
[1] Warren TK, et al. Nature. 2016 17;531(7594):381-5
[2] Agostini ML, et al. mBio. 2018 6;9(2)