| Hazard Information | Back Directory | [Uses]
BPR3P0128 is an orally active, non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that has been shown to inhibit the activity of various SARS-CoV-2 variants. The EC50 for SARS-CoV-2 and HCoV-229E are 0.62 μM and 0.14 μM. BPR3P0128 demonstrates effective anti-pancoronavirus activity within the submicromolar range. PR3P0128 shows synergistic antiviral activity when combined with Remdesivir (HY-104077)[1]. | [in vivo]
Pharmacokinetic Analysis in Sprague-Dawley rats Model[1]
| Route | Dose (mg/kg) | Cl (mL min/kg) | t1/2 (h) | F (%) | | i.v. | 0.01 | 1.3 | / | / | | p.o. | 0.01 | / | 8.1 | 78.7% |
| [References]
[1] Tang W-F, et al. BPR3P0128, a non-nucleoside RNA-dependent RNA polymerase inhibitor, inhibits SARS-CoV-2 variants of concern and exerts synergistic antiviral activity in combination with remdesivir. Antimicrob Agents Chemother. 2024;68(4):e0095623. DOI:10.1128/aac.00956-23
[2] Yeh JY, et al. Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization. ChemMedChem. 2012;7(9):1546-1550. DOI:10.1002/cmdc.201200259 |
|
|