BPR3P0128
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity : 98.58%
- CAS No.: 1345406-09-8
- Formula: C22H18BrN3O2
- Molecular Weight:436.30
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All DNA/RNA Synthesis Isoforms
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Biological Activity
Description
IC50 & Target
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RNA Polymerase |
In Vitro
BPR3P0128 (10 μM, 24 hours) can effectively inhibit the replication of SARS-CoV-2 in human lung cancer cell line Calu-3 and reduce the expression of cytokines induced by viral infection[1].
BPR3P0128 (1 μM, 10 μM) has comprehensive activity against coronavirus and can effectively inhibit different SARS-CoV-2 (including α, β, γ, δ, and plasmid strains) variants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Vero E6 cells containing SARS-CoV-2 virus
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Concentration:10 μM
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Incubation Time:0-24h
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Result:Significantly decreased the mRNA expression levels of CXCL10, IL-6, TNF-α and INF-β.
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Cell Line:Vero E6 cells containing SARS-CoV-2 virus
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Concentration:BPR3P0128: 1 μM, 2 μM; Remdesivir: 4 μM, 8 μM
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Incubation Time:24h
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Result:And Remdesivir synergistically inhibited NP expression more significantly.
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Cell Line:HEK293T cell-based RdRp reporter model
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Concentration:BPR3P0128: 0.1 μM, 1 μM, 10 μM; Remdesivir: 1 μM, 10 μM, 100 μM
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Incubation Time:24h
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Result:Inhibited the activity of SARS-CoV-2 RdRp, but did not decrease the expression level of nsp12.
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% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1345406-09-8
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Appearance Solid
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Molecular Weight 436.30
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Formula C22H18BrN3O2
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Color Light yellow to brown
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SMILES
O=C(O)C1=CC(C2=C(C)N(C3=CC(C)=CC=C3C)N=C2)=NC4=CC=C(Br)C=C41
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)