1. Anti-infection
  2. SARS-CoV
  3. BZ-30

BZ-30 is an orally active broad-spectrum SARS-CoV-2 inhibitor. BZ-30 acts on the early stage of the viral life cycle, can partially inhibit the endosomal entry process and reduce viral replication levels. BZ-30 reduces viral load, improves pulmonary pathological conditions, and decreases the lung-to-body weight ratio in hamster models challenged with SARS-CoV-2. BZ-30 can be used for research related to COVID-19.

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BZ-30

BZ-30 Chemical Structure

CAS No. : 3028405-31-1

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Description

BZ-30 is an orally active broad-spectrum SARS-CoV-2 inhibitor. BZ-30 acts on the early stage of the viral life cycle, can partially inhibit the endosomal entry process and reduce viral replication levels. BZ-30 reduces viral load, improves pulmonary pathological conditions, and decreases the lung-to-body weight ratio in hamster models challenged with SARS-CoV-2. BZ-30 can be used for research related to COVID-19[1].

In Vitro

BZ-30 (0.15-5 μM) reduces viral RNA levels by ≥99% in wild-type SARS-CoV-2-infected Vero E6 cells at the concentration of 5 μM, and exhibits dose-dependent antiviral activity[1].
BZ-30 (24 h) potently inhibits the effective replication of wild-type SARS-CoV-2 in Vero E6 cells, with an IC50 of 0.65 μM[1].
BZ-30 (24 h) acts as a broad-spectrum inhibitor of SARS-CoV-2 variants of concern in Vero E6 cells, with IC50 values ranging from 0.51 μM (Beta variant) to 12.37 μM (Omicron variant)[1].
BZ-30 can partially inhibit the endosomal entry of SARS-CoV-2 pseudovirus; its inhibitory effect is stronger in HEK293-ACE2 cells (up to 75%) compared with the 50% inhibition rate observed in HEK293-ACE2/TMPRSS2 cells[1].
BZ-30 (0-24 h) acts on the early stage of the wild-type SARS-CoV-2 life cycle in Vero E6 cells, and inhibits viral replication when administered within 2 h post-infection[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route Tmax Cmax AUC0-last AUC0-∞ Bioavailability T1/2 Vd CL
Mice[1] 5 mg/kg i.v. / / 711.9 nM·h 877.6 nM·h / 3.9 h 8.43 L/kg 1.89 L/h/kg
Mice[1] 10 mg/kg p.o. 0.5 h 5003.8 nM 1759.4 nM·h 3029.1 nM·h 100 % / / /
In Vivo

BZ-30 (15 mg/kg; i.p.; twice daily; 4 days starting 8 hours post-infection) reduces SARS-CoV-2 viral load by 64% and improves lung pathology in SARS-CoV-2-challenged Syrian golden hamsters[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Syrian Golden Hamsters (female, 6-8 weeks old, intranasally inoculated with 105 PFU of SARS-CoV-2)[1]
Dosage: 15 mg/kg
Administration: i.p.; twice daily; 4 days (starting 8 h post-infection)
Result: Reduced viral load by log10 0.44 TCID50 per mg lung, corresponding to a 64% reduction in viral load.
Significantly reduced the lung-to-body weight ratio.
Maintained body weight comparable to the positive control remdesivir.
Lowered the cumulative histopathological lung score from 14 to 3.
Showed minimal alveolar and epithelial cell degeneration, with only occasional peri-vascular and peri-bronchiolar focal inflammatory cell infiltration.
Molecular Weight

337.26

Formula

C14H13F6N3

CAS No.
SMILES

CC1(CCC1)NC2=NC3=C(C(F)(F)F)C=C(C(F)(F)F)C=C3N2

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • 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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BZ-30
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