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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- CAS No.: 2410688-60-5
- 화학식: C6H9FN2O5S
- 분자량:240.21
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보관:
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
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Beta-lactamase Isoforms
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Biological Activity
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2410688-60-5
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분자량 240.21
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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)
Pilabactam Related Classifications
HY-147349A Related Classifications
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