EIDD-1931 is a promising COVID-19 inhibitor. EIDD-1931 has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. In mice infected with SARS-CoV or MERS-CoV, both prophylactic and therapeutic administration of EIDD-2801, an orally bioavailable NHC-prodrug (β-D-N4-hydroxycytidine-5'-isopropyl ester), improved pulmonary function, and reduced virus titer and body weight loss. Decreased MERS-CoV yields in vitro and in vivo were associated with increased transition mutation frequency in viral but not host cell RNA, supporting a mechanism of lethal mutagenesis in CoV. The potency of NHC/EIDD-2801 against multiple coronaviruses and oral bioavailability highlight its potential utility as an effective antiviral against SARS-CoV-2 and other future zoonotic coronaviruses.EIDD-1931 is an active metabolite of EIDD-2801.
CAS Number: 3258-02-4
Molecular Weight: 259.22
Chemical Name: N4-Hydroxycytidine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Beta-d-N4-hydroxycytidine is an anti-VEEV (venezuelan equine encephalitis virus) agent with EC50, EC90, and EC99 are 0.426, 1.036, and 2.5 μM, respectively. Beta-d-N4-hydroxycytidine inhibits CHIKV replicon activity and the 50% effective concentration (EC50) s 0.8 μM in the Huh-7–CHIKV replicon cell line. Similar results is presented with the replicon in BHK-21 cells (EC50=1.8 μM). NHC has no cytotoxicity for NHC in the Huh-7 cell culture system until up to 100 μM using MTT assays. The 50% cytotoxic concentration (CCsub>50) values for NHC are determined to be 30.6 μM, 7.7 μM, and 2.5 μM in peripheral blood mononuclear (PBM), Vero, and CEM cells, respectively. NHC behaves as a pyrimidine analog, NHC-mediated inhibition of the CHIKV replicon can be abrogated by the addition of exogenous nucleosides, such as pyrimidines C and U, but dA, dC, dG, dU, or T has no impact on the replicon. Pyrimidines A and G contributes to replicon inhibition both in the presence and in the absence of NHC.
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