| Company Name: |
BOC Sciences |
| Tel: |
1-631-485-4226; 16314854226 |
| Email: |
info@bocsci.com |
|
| | 1H-Indole-2-carboxamide, 4-methoxy-N-[(1S)-3-methyl-1-[[[(1S)-2-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-3-(phosphonooxy)propyl]amino]carbonyl]butyl]- Basic information |
| | 1H-Indole-2-carboxamide, 4-methoxy-N-[(1S)-3-methyl-1-[[[(1S)-2-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-3-(phosphonooxy)propyl]amino]carbonyl]butyl]- Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: Soluble | | form | Solid | | color | White to off-white |
| | 1H-Indole-2-carboxamide, 4-methoxy-N-[(1S)-3-methyl-1-[[[(1S)-2-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-3-(phosphonooxy)propyl]amino]carbonyl]butyl]- Usage And Synthesis |
| Uses | Lufotrelvir (PF-07304814), a phosphate proagent of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle. | | Definition | ChEBI: PF-07304814 is an indolecarboxamide resulting from the formal condensation of the carboxy group of 4-methoxy-1H-indole-2-carboxylic acid with the primary amino group of N-[(2S)-3-oxo-1-[(3S)-2-oxopyrrolidin-3-yl]-4-(phosphonooxy)butan-2-yl]-L-leucinamide. It is the phosphate prodrug of PF-00835231, an anticoronaviral agent. It has a role as a prodrug, an EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor and an anticoronaviral agent. It is an aromatic ether, an indolecarboxamide, a secondary carboxamide, a member of pyrrolidin-2-ones, a L-leucine derivative and a phosphate monoester. It is functionally related to a PF-00835231. | | in vivo | Once administered through intravenous infusion, Lufotrelvir is cleaved into PF-00835231 to exert its anti-viral effects. Lufotrelvir exhibits a favorable cardiovascular safety profile[1].
Lufotrelvir is administered intravenously to rats, dogs and monkeys. It exhibits high systemic clearance and short half-life across species forming 68, 81, 76% PF-00835231 in rats, dogs and monkey respectively in comparison to the systemic exposure achieved with IV administration of PF00835231[1]. | | References | [1] Koen Vandyck, et al. Considerations for the discovery and development of 3-chymotrypsin-like cysteine protease inhibitors targeting SARS-CoV-2 infection. Curr Opin Virol. 2021 Apr 27;49:36-40. DOI:10.1016/j.coviro.2021.04.006
[2] Britton Boras, et al. Title: Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19 Short Title: Novel 3CL Protease Inhibitor for COVID-19
[3] BRITTON BORAS. Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19.[J]. ACS Combinatorial Science, 2021: 6055. DOI: 10.1038/s41467-021-26239-2 |
| | 1H-Indole-2-carboxamide, 4-methoxy-N-[(1S)-3-methyl-1-[[[(1S)-2-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-3-(phosphonooxy)propyl]amino]carbonyl]butyl]- Preparation Products And Raw materials |
|