1. Anti-infection
  2. SARS-CoV
  3. BPR3P0128

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).

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BPR3P0128 Chemical Structure

BPR3P0128 Chemical Structure

CAS No. : 1345406-09-8

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Based on 1 publication(s) in Google Scholar

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Description

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 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.

RT-PCR[1]

Cell Line: Vero E6 cells containing SARS-CoV-2 virus
Concentration: 10 μM
Incubation Time: 0-24h
Result: Significantly decreased the mRNA expression levels of CXCL10, IL-6, TNF-α and INF-β.

Western Blot Analysis[1]

Cell Line: Vero E6 cells containing SARS-CoV-2 virus
Concentration: BPR3P0128: 1 μM, 2 μM; Remdesivir: 4 μM, 8 μM
Incubation Time: 24h
Result: And Remdesivir synergistically inhibited NP expression more significantly.

Western Blot Analysis[1]

Cell Line: HEK293T cell-based RdRp reporter model
Concentration: BPR3P0128: 0.1 μM, 1 μM, 10 μM; Remdesivir: 1 μM, 10 μM, 100 μM
Incubation Time: 24h
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.

Molecular Weight

436.30

Formula

C22H18BrN3O2

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(O)C1=CC(C2=C(C)N(C3=CC(C)=CC=C3C)N=C2)=NC4=CC=C(Br)C=C41

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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BPR3P0128 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BPR3P0128
Cat. No.:
HY-161356
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