2. Others Anti-infection
  3. Drug Derivative Bacterial Beta-lactamase
  4. 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.

ATM potentiator-1

ATM potentiator-1 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

ATM potentiator-1 Related Antibodies

Top Publications Citing Use of Products

View All Beta-lactamase Isoform Specific Products:

View All Isoforms
Metallo-β-lactamase (MBL) Serine β-lactamase (SBL)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

In Vitro

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.

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 potentiators-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 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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

ATM potentiator-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 1Drug DerivativeBacterialBeta-lactamaseDrug derivativeβ-lactamaseHEK293 cellsPseudomonas aeruginosaβ-lactamase inhibitorKPC-2OXA-10OXA-48murine thigh infection modelNDM-1efflux pump inhibitorVIM-2Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ATM potentiator-1
Cat. No.:
HY-182058
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.