BC-2-Amp
BC-2-Amp is an antibiotic formed by conjugating Bis-catecholate with Ampicillin (HY-B0522). BC-2-Amp potently inhibits multidrug-resistant P. aeruginosa, with an MIC of 31.25 ng/mL against P. aeruginosa PA342. BC-2-Amp significantly broadens the antibacterial spectrum of Ampicillin against Gram-negative bacteria. BC-2-Amp utilizes the bis-catecholate siderophore to chelate Fe3+, specifically hijacking the P. aeruginosa outer membrane iron transport receptor (primarily PiuA) to penetrate the outer membrane barrier, delivering the β-lactam payload to the periplasmic space and targeting penicillin-binding proteins (PBPs) to exert bactericidal activity. BC-2-Amp can be used for research on infections caused by multidrug-resistant P. aeruginosa and other Gram-negative bacteria.
For research use only. We do not sell to patients.
- Formula: C36H40N6O11S
- Molecular Weight:764.80
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
β-lactam |
In Vitro
BC-2-Amp (4-8 μg/mL against PAO1; 1-2 μg/mL against PA342; 24 h/10 h) accelerates bacterial death in P. aeruginosa PAO1 and PA342 strains[1].
BC-2-Amp (1-4 μg/mL; 5-120 min) promotes intracellular iron uptake and accumulation in P. aeruginosa PAO1[1].
BC-2-Amp (4 μg/mL; 30 min) inhibits intracellular iron uptake in E. coli, A. baumannii, and K. pneumoniae[1].
BC-2-Amp (20 μg/mL; 20 min) significantly increases intracellular Amp accumulation in P. aeruginosa PAO1 and the mutant strain ΔpiuA[1].
BC-2-Amp (20 μg/mL; 20 min) increases intracellular Amp accumulation in PAO1 by 10-fold after 20 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:4, 8, 16, 32, 64, 128, 256, 512 g/mL
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Incubation Time:24 h
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Result:Showed negligible cytotoxicity toward HEK293T cells.
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Cell Line:P. aeruginosa PAO1 and its mutant ΔpiuA
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Concentration:20 μg/mL
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Incubation Time:20 min
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Result:Mediated a 10-fold increase in intracellular ampicillin accumulation compared to free ampicillin.
Upon treatment with a proton motive force uncoupler (CCCP) or in the absence of the PiuA receptor, ampicillin uptake was significantly reduced, verifying that its entry is an energy- and receptor-dependent active transport process.
In Vivo
BC-2-Amp (15 mg/kg; s.c.; single administration or once daily for 3 consecutive days) significantly reduces the bacterial burden at the infection site and decreases the area of skin lesions/ulcers in the BALB/c mouse P. aeruginosa lung infection model; a single 15 mg/kg subcutaneous dose reduces the skin PAO1 bacterial load by approximately 26-fold, and three 15 mg/kg doses reduce it by approximately 70-fold[1].
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, 6-8 weeks old)[1]
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Dosage:15 mg/kg (single-dose); 2 × 15 mg/kg (multiple-dose)
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Administration:i.n.; once at 0.5 h post-infection (single-dose); 2 doses over 2 days beginning at 0.5 h post-infection (multiple-dose)
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Result:Single-dose reduced lung bacterial burden from 1.4 × 10^7 CFU to 4.5 × 10^5 CFU (approximately 30-fold).
Multiple-dose reduced lung bacterial burden from 1.4 × 10^7 CFU to 1.1 × 10^5 CFU (over 100-fold).
Lung histological staining demonstrated efficacy.
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Animal Model:BALB/c (female, 6-8 weeks old)[1]
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Dosage:15 mg/kg (single-dose); 3 × 15 mg/kg (multiple-dose)
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Administration:s.c.; once at 0.5 h post-infection (single-dose); 3 doses over 3 days beginning at 0.5 h post-infection (multiple-dose)
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Result:Single-dose reduced skin bacterial burden from 1.6 × 10^7 CFU to 6.5 × 10^5 CFU (approximately 26-fold).
Multiple-dose reduced skin bacterial burden from 1.6 × 10^7 CFU to 2.3 × 10^5 CFU (approximately 70-fold).
Skin condition improved and bacterial load at infected sites was noticeably reduced.
Chemical Information
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Molecular Weight 764.80
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Formula C36H40N6O11S
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SMILES
O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC([C@@H](NC(CN(CCNC(C3=CC=CC(O)=C3O)=O)CCNC(C4=CC=CC(O)=C4O)=O)=O)C5=CC=CC=C5)=O)N1C2=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BC-2-Amp Related Classifications
HY-190839 Related Classifications
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Keywords
- BC-2-Amp
- Antibiotic
- Drug Derivative
- Penicillin-binding protein (PBP)
- Bacterial
- Drug derivative
- PiuA
- Pseudomonas aeruginosa
- TonB-dependent uptake
- cell wall synthesis
- ferric iron chelation
- multidrug-resistant
- murine lung infection
- murine skin infection
- penicillin-binding proteins
- siderophore-mediated uptake
- Inhibitor
- inhibitor
- inhibit