2. Anti-infection
  3. Beta-lactamase
  4. ATM potentiator-1

ATM potentiator-1 (compound 9) is a β-lactamase inhibitor and efflux pump inhibitor, with an IC50 of 1.6 μM against NDM-1, IC50 values of 12.5 μM and 5.4 μM against OXA-10, an IC50 of 5.0 μM against VIM-2, an IC50 of 26.7 μM against KPC-2, and an IC50 of 3.4 μM against OXA-48. ATM potentiator-1 inhibits the efflux pump activity of *Pseudomonas aeruginosa* and exerts a synergistic inhibitory effect when combined with CCCP. ATM potentiators-1 can be used for the research of carbapenem-resistant *Pseudomonas aeruginosa* (CRPA) infections.

For research use only. We do not sell to patients.

ATM potentiator-1

ATM potentiator-1 Chemical Structure

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ATM potentiator-1 Related Antibodies

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Description

ATM potentiator-1 (compound 9) is a β-lactamase inhibitor and efflux pump inhibitor, with an IC50 of 1.6 μM against NDM-1, IC50 values of 12.5 μM and 5.4 μM against OXA-10, an IC50 of 5.0 μM against VIM-2, an IC50 of 26.7 μM against KPC-2, and an IC50 of 3.4 μM against OXA-48. ATM potentiator-1 inhibits the efflux pump activity of *Pseudomonas aeruginosa* and exerts a synergistic inhibitory effect when combined with CCCP. ATM potentiators-1 can be used for the research of carbapenem-resistant *Pseudomonas aeruginosa* (CRPA) infections[1].

In Vitro

ATM potentiator-1 (compound 9) (0.1, 1, 10, 70 μM; 20 min) 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 potentiator-1 (0, 10, 25, 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 potentiator-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 potentiator-1 (16 mg/L; 24 h) potentiates aztreonam activity against NDM-1-producing Pseudomonas aeruginosa strain PA-017, reducing the aztreonam MIC from 16 mg/L to 1 mg/L[1].
ATM potentiator-1 (1, 2, 4, 8, 16, 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].
ATM potentiator-1 (1, 2, 4, 8, 16, 32 mg/L) does not permeabilize the outer membrane of NDM-1-producing Pseudomonas aeruginosa strain PA-017, as shown by unchanged NPN fluorescence[1].
ATM potentiator-1 (0.5, 1, 2, 4, 8, 16, 32 mg/L; 24 h) does not reduce the viability of immortalized human embryonic kidney HEK293 cells after 24 h of incubation[1].
ATM potentiator-1 (4, 8, 16, 32 mg/L; 30 min) does not cause hemolysis of human red blood cells after 30 min of incubation at 37 °C[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ATM potentiator-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: Immortalized human embryonic kidney (HEK293) cells
Concentration: 0.5, 1, 2, 4, 8, 16, 32 mg/L
Incubation Time: 24 h
Result: Did not affect HEK293 cell viability at concentrations up to 32 mg/L.
Parmacokinetics
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
In Vivo

ATM potentiator-1 (compound 9) (40 mg/kg; i.p.; 4 total doses at 2-hour intervals, in combination with 20 mg/kg aztreonam) achieves a 3.4 log10 reduction in bacterial burden in a murine thigh infection model with NDM-1-producing Pseudomonas aeruginosa[1].
ATM potentiator-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.

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]
Dosage: 40 mg/kg (in combination with 20 mg/kg aztreonam)
Administration: i.p.; 4 total doses at 2-hour intervals
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.
Animal Model: C57BL/6J mice (6 week-old female)[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.p.; single dose
Result: Resulted in 100% survival of mice over the 7-day observation period for all doses.
Molecular Weight

472.44

Formula

C23H22F2N4O5
SMILES

OC1=C2C(C(OCCC(C)(C)C)=C(OC2=CC(OCC3=NN=NN3)=C1)C4=CC=C(C(F)=C4)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ATM potentiator-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ATM potentiator-1ATM potentiator1ATM potentiator 1Beta-lactamaseβ-lactamaseHEK293 cellsPseudomonas aeruginosaβ-lactamase inhibitorKPC-2OXA-10OXA-48murine thigh infection modelNDM-1efflux pump inhibitorVIM-2Inhibitorinhibitorinhibit

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