ATM potentiator-1
ATM potentiators-1 is a quercetin derivative that synergistically enhances the antibacterial activity of Aztreonam (ATM, HY-B0129) against metallo-β-lactamase-producing Pseudomonas aeruginosa. ATM potentiators-1 inhibits NDM-1, OXA-10, VIM-2, KPC-2, and OXA-48, suppressing the efflux pump activity of Pseudomonas aeruginosa. When used in combination with CCCP (HY-100941), it exhibits a synergistic inhibitory effect. ATM potentiators-1 is applicable to research related to Pseudomonas aeruginosa infections.
For research use only. We do not sell to patients.
- Formula: C23H22F2N4O5
- Molecular Weight:472.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Beta-lactamase Isoforms
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Biological Activity
ATM potentiators-1 (compound 9) inhibits purified β-lactamases KPC-2, NDM-1, VIM-2, OXA-48, and OXA-10 with IC50 values ranging from 1.6 to 26.7 μM, with the strongest activity against NDM-1[1].
ATM potentiators-1 (0-50 μM; 10 min) binds to the active site of purified NDM-1, as shown by concentration-dependent quenching of intrinsic tryptophan fluorescence[1].
ATM potentiators-1 (8 mg/L; 60 min) inhibits efflux pumps in NDM-1-producing Pseudomonas aeruginosa strain PA-017, as indicated by enhanced intracellular retention of ethidium bromide[1].
ATM potentiators-1 (16 mg/L; 24 h) potentiates aztreonam activity against NDM-1-producing Pseudomonas aeruginosa strain PA-017[1].
ATM potentiators-1 (1-32 mg/L; 18-24 h) potentiates aztreonam activity against 29 carbapenemase-producing carbapenem-resistant Pseudomonas aeruginosa isolates, with 93% showing synergistic interaction (FICI ≤0.5) and a ≥4-fold reduction in aztreonam MIC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Immortalized human embryonic kidney (HEK293) cells
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Concentration:0.5, 1, 2, 4, 8, 16, 32 mg/L
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Incubation Time:24 h
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Result:Did not affect HEK293 cell viability at concentrations up to 32 mg/L.
| Species | Dose | Route | T1/2 | Cmax | AUC0-last | AUC0-∞ | MRT0-last | MRT0-∞ | C0 | Vss | Vz | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 1.44 h | 6.96 mg/L | 2.55 mg·h/L | 2.61 mg·h/L | 0.63 h | 0.85 h | 13.23 mg/L | 3.45 L/kg | 1.00 L/kg | 2000 mL/h/kg |
ATM potentiators-1 (10-40 mg/kg; i.p.; single dose) is well-tolerated in 6 week-old female C57BL/6J mice, with 100% survival over 7 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (7 week-old female, 20-22 g, intramuscular thigh infection with NDM-1-producing Pseudomonas aeruginosa strain PA-017)[1]
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Dosage:40 mg/kg (in combination with 20 mg/kg aztreonam)
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Administration:i.p.; 4 total doses at 2-hour intervals
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Result:Reduced mean bacterial burden in thigh tissue to 4.26 log10 CFU/thigh, representing a 3.4 log10 drop compared to untreated control.
Achieved a greater reduction than aztreonam alone (2.2 log10 drop).
Reduced thigh muscle weight by 26.4% compared to untreated control.
Caused no significant body weight changes or overt clinical signs.
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Animal Model:C57BL/6J mice (6 week-old female)[1]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.p.; single dose
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Result:Resulted in 100% survival of mice over the 7-day observation period for all doses.
Chemical Information
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Molecular Weight 472.44
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Formula C23H22F2N4O5
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SMILES
OC1=C2C(C(OCCC(C)(C)C)=C(OC2=CC(OCC3=NN=NN3)=C1)C4=CC=C(C(F)=C4)F)=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)
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