CAS Number: 1809249-37-3
Formula: C27H35N6O8P
Molecular Weight: 602.585 g·mol−1
Method of analysis:In House
Pharmacology
Remdesivir is indicated for the treatment of coronavirus disease 2019 (COVID‑19) in adults and adolescents (aged twelve years and older with body weight at least 40 kg) with pneumonia requiring supplemental oxygen. Remdesivir is a ProTide (Prodrug of nucleoTide). It is able to diffuse into cells where it is converted to GS-441524 mono-phosphate via the actions of esterases (CES1 and CTSA) and a phosphoamidase (HINT1); this in turn is further phosphorylated to its active metabolite triphosphate by nucleoside-phosphate kinases. This pathway of bioactivation is meant to occur intracellularly, but a substantial amount of remdesivir is prematurely hydrolyzed in plasma, with GS-441524 being the major metabolite in plasma, and the only metabolite remaining two hours after dosing.
Mechanism
As an adenosine nucleoside triphosphate analog (GS-443902), the active metabolite of remdesivir interferes with the action of viral RNA-dependent RNA polymerase and evades proofreading by viral exoribonuclease (ExoN), causing a decrease in viral RNA production. In some viruses such as the respiratory syncytial virus it causes the RNA-dependent RNA polymerases to pause, but its predominant effect (as in Ebola) is to induce an irreversible chain termination. Unlike with many other chain terminators, this is not mediated by preventing addition of the immediately subsequent nucleotide, but is instead delayed, occurring after five additional bases have been added to the growing RNA chain. For the RNA-Dependent RNA Polymerase of MERS-CoV, SARS-CoV-1, and SARS-CoV-2 arrest of RNA synthesis occurs after incorporation of three additional nucleotides. Hence, remdesivir is classified as a direct-acting antiviral agent that works as a delayed chain terminator.
Storage Condition: preserve in well-closed containers, protect from moisture at controlled room temperature.
Packaging:Vial