For research use only. Not for therapeutic Use.
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)[1][2].
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[2].
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[2].
Bofutrelvir exhibits an additive effect against SARS-CoV-2 in vitro when combined treatment with remdesivi[2].
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[2].
| Catalog Number | I032743 |
| CAS Number | 2103278-86-8 |
| Synonyms | N-[(2S)-3-cyclohexyl-1-oxo-1-[[(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl]amino]propan-2-yl]-1H-indole-2-carboxamide |
| Molecular Formula | C25H32N4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H32N4O4/c30-15-19(13-18-10-11-26-23(18)31)27-24(32)21(12-16-6-2-1-3-7-16)29-25(33)22-14-17-8-4-5-9-20(17)28-22/h4-5,8-9,14-16,18-19,21,28H,1-3,6-7,10-13H2,(H,26,31)(H,27,32)(H,29,33)/t18-,19-,21-/m0/s1 |
| InChIKey | HPKJGHVHQWJOOT-ZJOUEHCJSA-N |
| SMILES | C1CCC(CC1)CC(C(=O)NC(CC2CCNC2=O)C=O)NC(=O)C3=CC4=CC=CC=C4N3 |
| Reference | [1]. Ullrich S, Nitsche C. The SARS-CoV-2 main protease as drug target. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127377. [2]. Shang W, et al. In vitro and in vivo evaluation of the main protease inhibitor FB2001 against SARS-CoV-2. Antiviral Res. 2022 Dec;208:105450. |
