Pilabactam
Pilabactam (ANT3310) is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam can be used in the research of bacterial infection.
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- No. CAS: 2410688-60-5
- Fòrmula: C6H9FN2O5S
- Peso molecular:240.21
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
Pilabactam (Compound 21, 0.006 to 3 000 nM, 10 min) inhibits a series of Serine β-Lactamase (AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2), with IC50 values ranging from 1 nM to 175 nM[1].
Pilabactam shows a low in vitro cytotoxicity (IC<>50: > 100 μM) in HepG2 cell, cardiotoxicity (inhibition of the hERG potassium ion channel), and genotoxicity (Ames test)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Pilabactam (intravenous injection, 1 mg/kg, Male Swiss albino mice) shows a T1/2 value of 0.64 h, AUC value of 412 ng•h/mL, and Cl value of 40 mL/min/kg (pharmacokinetic assay)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine thigh infection model[1]
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Dosage:25, 50, and 100 mg/kg
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Administration:Intravenous injection, at 1, 3, 5, and 7 h postinfection
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Result:Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2410688-60-5
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Peso molecular 240.21
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Fòrmula C6H9FN2O5S
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SMILES
O=S(ON1[C@H]2C[N@]([C@@H](CC2)F)C1=O)(O)=O
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Synonyms
ANT3310
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
Referencias
[1]. David T Davies, et al. Discovery of ANT3310, a Novel Broad-Spectrum Serine β-Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii. J Med Chem. 2020 Dec 24;63(24):15802-15820. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)