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]-
- Product Name
- 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]-
- CAS No.
- 2468015-78-1
- Chemical Name
- 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]-
- Synonyms
- Lufotrelvir;Lufotrelvir (PF-07304814);Lufotrelvir (PF-07304814) ，S9858;(S)-3-((S)-2-(4-Methoxy-1H-indole-2-carboxamido)-4-methylpentanamido)-2-oxo-4-((S)-2-oxopyrrolidin-3-yl)butyldihydrogenphosphate;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]-
- CBNumber
- CB18097634
- Molecular Formula
- C24H33N4O9P
- Formula Weight
- 552.51
- MOL File
- 2468015-78-1.mol
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]- Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: Soluble
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- SML3315
- Product name
- PF-07304814
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $67.54
- Updated
- 2025/07/31
- Product number
- SML3315
- Product name
- PF-07304814
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $288
- Updated
- 2025/07/31
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,Usage,Production
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
Raw materials
Preparation Products
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