Molnupiravir (EIDD-2801)

Synonyms: MK-4482

Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19.

Molnupiravir (EIDD-2801) Chemical Structure

Molnupiravir (EIDD-2801) Chemical Structure

CAS No. 2349386-89-4

Purity & Quality Control

Molnupiravir (EIDD-2801) Related Products

Biological Activity

Description Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19.
Targets
SARS-CoV-2 [1] MERS-CoV [1] SARS-CoV [1]
In vitro
In vitro

EIDD-2801 is an orally bioavailable NHC-prodrug. NHC is potently antiviral against SARS-CoV-2, MERS-CoV and SARS-CoV in primary human epithelial cell cultures without cytotoxicity. NHC is effective against remdesivir (RDV)-resistant vi-rus and multiple distinct zoonotic CoV. NHC antiviral activity is associated with increased viral mutation rates.[1]

In Vivo
In vivo

EIDD-2801 is efficiently hydrolyzed in vivo after absorption, resulting in detection of only free NHC in plasma.[2]

Therapeutic EIDD-2801 is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit is dependent on the time of initiation post-infection. EIDD-2801 robustly reduces MERS-CoV infectious titers, viral RNA, and pathogenesis under both prophylactic and early therapeutic conditions.[1]

Animal Research Animal Models 20-29 week old SPF C57BL/6J mice, 10-14 week old C57BL/6J hDPP4 mice
Dosages 50 mg/kg, 150 mg/kg, 500 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04405739 Completed
SARS-CoV 2
Ridgeback Biotherapeutics LP|Merck Sharp & Dohme LLC
June 16 2020 Phase 2

Chemical Information & Solubility

Molecular Weight 329.31 Formula

C13H19N3O7

CAS No. 2349386-89-4 SDF --
Smiles CC(C)C(=O)OCC1C(C(C(O1)N2C=CC(=NC2=O)NO)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 66 mg/mL ( (200.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 22 mg/mL

Water : 20 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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