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Remdesivir and GS-441524 a ProDrug

Reference Number: AA-04138 Created: 06/05/2020 01:36 PM Last Updated: 09/05/2020 10:00 AM

Method Conditions:

Column: Cogent Diamond Hydride™, 4 μm, 100 Å 
Catalog No.: 70000-75P
Dimensions: 4.6 x 75mm
Solvents: A. DI H20 / 0.1% formic acid (v/v)
                B. Acetonitrile / 0.1% formic acid (v/v)
Isocratic:  92% B
Injection Volume: 2ul
Flow Rate: 1.0 mL / min
Detection: 254 nm
Peak: 1. Remdesivir
          2. GS-441524 

Samples: Remdesivir and GS-441524 in 0.1 mg/mL concentration

Discussion: Remdesivir, an antiviral drug, and GS-441524, a pro-drug converted in the body as a ribonucleotide analog, is as a mixture that may be difficult to analyze in routine chromatographic analysis.  As GS-441524 is polar, is makes it more difficult to retain in typical reversed phase conditions.  By use of the Cogent Diamond Hydride™ column in ANP, we have illustrated how this contrasting mixture of compounds can be retained and still possess excellent peak shape.  This method demonstrates an easy HPLC method that can be easily transferred to LCMS.  

Note: Remdesivir is a broad-spectrum antiviral drug that is able to diffuse into cells where it is converted to GS-441524 mono-phosphate.  This achieved via the actions of esterases and a phosphoamidase; which in turn is further phosphorylated to its active metabolite triphosphate by nucleoside-phosphate kinases GS-441524.  GS-441524 has previously been researched as a treatment for feline infectious peritonitis (FIP), a lethal coronavirus disease which affects domestic cats.

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