BLI-489
Based on 1 Customer Validation
BLI-489 is a Beta-lactamase inhibitor. BLI-489 is an antibacterial adjuvant that significantly enhances the antibacterial efficacy of β-lactam antibiotics. BLI-489 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 can be used for research on bacterial infections.
For research use only. We do not sell to patients.
- Purity : 95.77%
- CAS No.: 623564-40-9
- Formula: C13H10N3NaO4S
- Molecular Weight:327.29
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Beta-lactamase Isoforms
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Biological Activity
Description
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NDM-1 |
AmpC |
In Vitro
BLI-489 (2-4 μg/mL; 18-22 h) 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) 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) 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) exhibits synergistic antibacterial activity with Imipenem (HY-B1369A) in CRAb strains producing CHDLs and MBLs[2].
BLI-489 (8 mg/L; 6-24 h) 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) 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) 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) 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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 623564-40-9
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Appearance Solid
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Molecular Weight 327.29
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Formula C13H10N3NaO4S
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Color Light yellow to yellow
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SMILES
O=C(C1=CS[C@@](/C2=C/C3=CN4C(COCC4)=N3)([H])N1C2=O)O[Na]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : ≥ 105 mg/mL (320.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0554 mL | 15.2770 mL | 30.5539 mL | 76.3849 mL |
| 5 mM | 0.6111 mL | 3.0554 mL | 6.1108 mL | 15.2770 mL | |
| 10 mM | 0.3055 mL | 1.5277 mL | 3.0554 mL | 7.6385 mL | |
| 15 mM | 0.2037 mL | 1.0185 mL | 2.0369 mL | 5.0923 mL | |
| 20 mM | 0.1528 mL | 0.7638 mL | 1.5277 mL | 3.8192 mL | |
| 25 mM | 0.1222 mL | 0.6111 mL | 1.2222 mL | 3.0554 mL | |
| 30 mM | 0.1018 mL | 0.5092 mL | 1.0185 mL | 2.5462 mL | |
| 40 mM | 0.0764 mL | 0.3819 mL | 0.7638 mL | 1.9096 mL | |
| 50 mM | 0.0611 mL | 0.3055 mL | 0.6111 mL | 1.5277 mL | |
| 60 mM | 0.0509 mL | 0.2546 mL | 0.5092 mL | 1.2731 mL | |
| 80 mM | 0.0382 mL | 0.1910 mL | 0.3819 mL | 0.9548 mL | |
| 100 mM | 0.0306 mL | 0.1528 mL | 0.3055 mL | 0.7638 mL |
BLI-489 Related Classifications
HY-108062 Related Classifications
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Keywords
- BLI-489
- 623564-40-9
- 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