BPR3P0128 is an orally active non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that can inhibit the activity of various SARS-CoV-2 variants, with EC50 of 0.62 and 0.14 µM for SARS-CoV-2 and HCoV-229E, respectively. BPR3P0128 has potent anti-pan-coronavirus activity in the submicromolar range. BPR3P0128 exhibits synergistic antiviral activity when used in combination with Remdesivir.

Physicochemical Properties

Molecular Formula	C22H18BRN3O2
Molecular Weight	436.30
CAS #	1345406-09-8
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	BPR3P0128 (10 μM, 24 hours) can effectively inhibit the replication of SARS-CoV-2 in the human lung cancer cell line Calu-3 and reduce the expression of cytokines caused by viral infection[1]. BPR3P0128 (1 μM, 10 μM) has comprehensive activity against coronaviruses and can effectively inhibit different SARS-CoV-2 (including α, β, γ, δ and mycoplasmic strains) variants[1]. BPR3P0128 (1 μM, 2 μM; 24 hours) exhibits synergistic antiviral activity when used in combination with Remdesivir (4 μM, 8 μM)[1].
Cell Assay	RT-PCR[1] Cell Types: Vero E6 cells containing SARS-CoV-2 virus Tested Tested Concentrations: 10 μM Incubation Duration: 0-24h Experimental Results: Significantly decreased the mRNA expression levels of CXCL10, IL-6, TNF-α and INF-β. Western Blot Analysis[1] Cell Types: Vero E6 cells containing SARS-CoV-2 virus Tested Tested Concentrations: BPR3P0128: 1 μM, 2 μM; Remdesivir: 4 μM, 8 μM Incubation Duration: 24h Experimental Results: And Remdesivir synergistically inhibited NP expression more significantly. Western Blot Analysis[1] Cell Types: HEK293T cell-based RdRp reporter model Tested Tested Concentrations: BPR3P0128: 0.1 μM, 1 μM, 10 μM; Remdesivir: 1 μM, 10 μM, 100 μM Incubation Duration: 24h Experimental Results: Inhibited the activity of SARS-CoV-2 RdRp, but did not decrease the expression level of nsp12.
References	[1]. 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. [2]. Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization. ChemMedChem. 2012;7(9):1546-1550.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2920 mL	11.4600 mL	22.9200 mL
	5 mM	0.4584 mL	2.2920 mL	4.5840 mL
	10 mM	0.2292 mL	1.1460 mL	2.2920 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.