BLI-489 free base
BLI-489 free base is a Beta-lactamase inhibitor. BLI-489 free base is an antibacterial adjuvant that significantly enhances the antibacterial efficacy of β-lactam antibiotics. BLI-489 free base blocks the hydrolytic activity of the enzyme by forming a stable intermediate in serine Beta-lactamase, or by coordinating with the binuclear Zn2+ through an oxygen atom in metallo-Beta-lactamase. BLI-489 free base can be used for research on bacterial infections.
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- CAS. Nr.: 635322-76-8
- Formel: C13H11N3O4S
- Molecular Weight:305.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
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NDM-1 |
AmpC |
In Vitro
BLI-489 (2-4 μg/mL; 18-22 h) free base enhances the antibacterial activity of Piperacillin (HY-B1923) against various predicted panels of Gram-negative and Gram-positive bacteria and clinical isolates[1].
BLI-489 (up to 64 µg/mL; 24 h) free base exhibits synergistic growth inhibition with Ceftriaxone (HY-B0712) in NDM-producing NDM-Kp, with an MIC of 8 μg/mL and an MBC of 16 μg/mL[4].
BLI-489 (4-16 μg/mL; 4-24 h) free base inhibits biofilm formation in NDM-Kp, does not cause bacterial cell membrane protein leakage, reduces bacterial load, and maintains the integrity of cell surface morphology[4].
BLI-489 (8 mg/L; 24 h) free base exhibits synergistic antibacterial activity with Imipenem (HY-B1369A) in CRAb strains producing CHDLs and MBLs[2].
BLI-489 (8 mg/L; 6-24 h) free base in combination with Imipenem shows synergy against OXA-24-like, OXA-51-like, and OXA-58-producing CRAb isolates, but does not show synergy against OXA-23-producing CRAb isolates after 24 h[2].
BLI-489 (4-64 μg/mL; 4 h) free base exhibits low hemolytic activity and high biocompatibility in red blood cells (RBCs)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NDM-producing Klebsiella pneumoniae
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Concentration:4 μg/mL, 8 μg/mL
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Incubation Time:24 h
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Result:Significantly reduced the number of bacterial colonies within 24 hours and continuously inhibited the regrowth of the bacteria in combination with Ceftriaxone.
In Vivo
BLI-489 (ED50 dose in combination with Piperacillin ranges from 8.5-69 mg/kg; s.c.; administered at 30 min and 150 min post-infection, 1-2 doses total; observed for 7 days after the first day of dosing) free base significantly improves survival rates and restores the in vivo efficacy of Piperacillin in CD-1 mouse acute lethal systemic infection models caused by various β-lactamase-producing pathogenic bacteria[3].
BLI-489 (8 mg/L; administered in agar medium; single administration; 24 h) free base synergizes with Imipenem to improve nematode survival in the CRAb-infected C. elegans model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-7 weeks old, 20-25 g)[2]
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Dosage:25 mg/kg (alone); 25 mg/kg (combination with Imipenem 25 mg/kg)
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Administration:i.p.; every 8 h; 3 days
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Result:Rescued 76.7% of mice from CRAb pneumonia in combination with Imipenem.
BLI-489 alone resulted in significantly higher activity against AbTVGH-908 than Imipenem alone.
Chemical Information
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CAS. Nr. 635322-76-8
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Molecular Weight 305.31
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Formel C13H11N3O4S
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SMILES
OC(C1=CS[C@@](/C2=C\C3=CN4C(COCC4)=N3)([H])N1C2=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Petersen PJ, et al. Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489. Antimicrobial agents and chemotherapy. 2009 Feb;53(2):370-84. [Content Brief]
[2]. Wang YC, et al. In vitro and in vivo activities of imipenem combined with BLI-489 against class D β-lactamase-producing Acinetobacter baumannii. The Journal of antimicrobial chemotherapy. 2021 Jan 19;76(2):451-459. [Content Brief]
[3]. Petersen PJ, et al. Efficacy of piperacillin combined with the Penem beta-lactamase inhibitor BLI-489 in murine models of systemic infection. Antimicrobial agents and chemotherapy. 2009 Apr;53(4):1698-700. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BLI-489 free base Related Classifications
HY-108062B Related Classifications
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Keywords
- BLI-489
- 635322-76-8
- BLI489
- BLI 489
- Beta-lactamase
- Bacterial
- OXA-24-like and OXA-58-like β-lactamases
- New Delhi metallo-β-lactamase
- Klebsiella pneumoniae
- methicillin-susceptible staphylococci
- class A
- class C
- and class D β-lactamases
- penem β-lactamase inhibitor
- Cys208
- His250
- and Asp124
- Acinetobacter baumannii
- biofilm formation
- carbapenemase-producing isolates
- Inhibitor
- inhibitor
- inhibit