Bofutrelvir

Research use only, not for human use.

Bofutrelvir (FB2001) is a SARS-CoV-2 3CL protease inhibitor with antiviral activity for the study of novel coronavirus pneumonia (COVID-19) infections.

Bofutrelvir (FB2001) is a SARS-CoV-2 main protease Mpro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077).

Bofutrelvir (24 h) shows in vitro activity against SARS-CoV-2 and its variants with EC50 values of 0.42, 0.39, 0.28, 0.27 and 0.26 μM for SARS-CoV-2, SARS-CoV-2 (Alpha), SARS-CoV-2 (Beta), SARS-CoV-2 (Delta) and SARS-CoV-2 (Omicron), respectively. Bofutrelvir inhibits SARS-CoV-2 replication in vero E6 cells in the presence of human serum (1.1-2.4 μM) even at the dose of EC50 values.Bofutrelvir exhibits an additive effect against SARS-CoV-2 in vitro when combined treatment with remdesivi.

Bofutrelvir (100 and 200 mg/kg; i.p. once daily on day 0 and twice daily on day 1, 2 and 3 for 4 consecutive days) effectively against SARS-CoV-2 delta variant infection in vivo.Animal Model:K18-hACE2 mice with SARS-CoV-2 delta variant infection Dosage:100 and 200 mg/kg Administration:Intraperitoneal injection; 100 and 200 mg/kg once daily on day 0 and twice daily on day 1, 2 and 3 for 4 consecutive days Result:Showed a dose-dependent efficacy to virus titers of lung. Effectively reduces the lung viral loads. Dose-dependently showed antiviral activity against the SARS-CoV-2 Delta variant and significantly reduced viral load in mouse lung and brain.

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Others

Other Targets

SARS-CoV

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2103278-86-8

452.55

C25H32N4O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (220.97 mM; Ultrasonic )

C(N[C@@H](CC1CCCCC1)C(N[C@@H](C[C@H]2C(=O)NCC2)C=O)=O)(=O)C3=CC=4C(N3)=CC=CC4

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(-20℃)

With Ice Pack

≥ 2 years