2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Anti-infection Cell Cycle/DNA Damage
  3. Reactive Oxygen Species (ROS) Bacterial ClpP
  4. Anti-MRSA agent 39

Anti-MRSA agent 39 is an orally active ClpX modulator that binds Staphylococcus aureus caseinolytic protease X (SaClpX) with high affinity (Kd = 3.6 μM). Anti-MRSA agent 39 exerts antibacterial effects through temperature-dependent inhibition of cell division. Anti-MRSA agent 39 elicits profound metabolic dysregulation in methicillin-resistant Staphylococcus aureus (MRSA), manifesting as significantly reduced ATP levels, elevated reactive oxygen species (ROS), and decreased NAD+/NADH ratio, and accelerates bacterial lysis rates in MRSA ATCC 33591. Anti-MRSA agent 39 significantly increases the proportion of MRSA cells in the mitotic phase, and the cells exhibit obvious morphological abnormalities. Anti-MRSA agent 39 can be used for the study of invasive MRSA infections.

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Anti-MRSA agent 39

Anti-MRSA agent 39 Chemical Structure

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Anti-MRSA agent 39 Related Antibodies

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Description

Anti-MRSA agent 39 is an orally active ClpX modulator that binds Staphylococcus aureus caseinolytic protease X (SaClpX) with high affinity (Kd = 3.6 μM). Anti-MRSA agent 39 exerts antibacterial effects through temperature-dependent inhibition of cell division. Anti-MRSA agent 39 elicits profound metabolic dysregulation in methicillin-resistant Staphylococcus aureus (MRSA), manifesting as significantly reduced ATP levels, elevated reactive oxygen species (ROS), and decreased NAD+/NADH ratio, and accelerates bacterial lysis rates in MRSA ATCC 33591. Anti-MRSA agent 39 significantly increases the proportion of MRSA cells in the mitotic phase, and the cells exhibit obvious morphological abnormalities. Anti-MRSA agent 39 can be used for the study of invasive MRSA infections[1].

In Vitro

Anti-MRSA agent 39 (Compound 13) (18-72 h) demonstrates potent inhibitory activity against MRSA (MIC = 1 μg/mL) and does not show significant toxicity to human liver cell line LO2 (IC50 = 8.15 μM)[1].
Anti-MRSA agent 39 (0.25-1 μg/mL, 0-12 h) can rapidly eliminate MRSA in a concentration-dependent manner and reduce the bacterial load to an undetectable level within 12 h at 4 × MIC[1].
Anti-MRSA agent 39 exhibits a significantly lower propensity for inducing resistance mutations compared to vancomycin[1].
Anti-MRSA agent 39 (100 μM, 30 min) stabilizes the SaClpX hexamer structure and reduces dimer/trimer formation[1].
Anti-MRSA agent 39 significantly upregulates ftsZ mRNA expression levels in MRSA ATCC 33591[1].
Anti-MRSA agent 39 exhibits a 2-4 fold decrease in MIC at 30°C, the "negative temperature coefficient" characteristic consistent with the activity of the ClpX chaperone in MRSA ATCC 33591[1].
Anti-MRSA agent 39 (0.25-0.5 μg/mL, 1-5 h) elicits profound metabolic dysregulation in MRSA, manifesting as significantly reduced ATP levels, elevated reactive oxygen species (ROS), and decreased NAD+/NADH ratio, and accelerates bacterial lysis rates in MRSA ATCC 33591[1].

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

Anti-MRSA agent 39 Related Antibodies
In Vivo

Anti-MRSA agent 39 (Compound 13) (5-1000 mg/kg, p.o., once; s.c., once daily for 3 days) significantly reduces bacterial load and lesion size in a mouse MRSA skin infection model, effectively inhibits MRSA infection, promotes wound healing, and shows good safety at doses ≤ 750 mg/kg[1].

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

Animal Model: Male BALB/c mice (8-week-old)[1].
Dosage: 500 mg/kg, 750 mg/kg, 1000 mg/kg
Administration: P.o., once
Result: A decrease in body weight on the second day and a 50 % mortality rate were observed within the first five days.
At the doses of 750 mg/kg and 500 mg/kg, no toxic reactions or mortalities were observed throughout the experiment.
The 750 mg/kg dosage group demonstrated a transient decrease in body weight on the second day; subsequently, their body weights gradually recovered from the fifth day post-administration.
Showed mild liver and kidney inflammation in the 1000 mg/kg and 750 mg/kg dose groups.
No significant organ damage in the major organs of the mice.
Animal Model: A skin abscess model was established in male BALB/c mice (8-week-old) by subcutaneous injection of 60 μL of MRSA bacterial suspension (1 × 107 CFU/mL)[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: S.c., once daily for 3 days
Result: Exhibited a substantial recovery in body weight, enhanced wound healing, and a significant reduction in lesion size and subsidence rate.
Exhibited a reduction in bacterial content within the skin of the mice.
Exhibited no discernible pathological alterations, maintaining a well-defined skin structure and minimal inflammatory cell infiltration.
Molecular Weight

338.20

Formula

C18H12BrNO
SMILES

O=C(C1=CC=CC=C1Br)/C=C/C2=NC3=CC=CC=C3C=C2
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
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Anti-MRSA agent 39 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:

Anti-MRSA agent 39Reactive Oxygen Species (ROS)BacterialClpPCaseinolytic protease PMethicillin-Resistant Staphylococcus aureusMRSAClpXInhibitorinhibitorinhibit

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