ClpP agonist 1
ClpP agonist 1 is a Staphylococcus aureus ClpP (SaClpP) agonist with an EC50 of 1.44 μM, Kd values of 2.95 μM (isothermal titration calorimetry) and 18 μM (bio-layer interferometry), and a low drug resistance frequency. ClpP agonist 1 reduces bacterial load, shrinks infected area and improves histopathological outcomes in a mouse skin infection model. ClpP agonist 1 can be used for the research of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) skin infections.
For research use only. We do not sell to patients.
- CAS No.: 2761081-10-9
- Formula: C24H21F5N4O
- Molecular Weight:476.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
ClpP agonist 1 (Compound Z1) (0.06-128 μg/mL; 18 h) exhibits potent antibacterial activity against MRSA ATCC 33591 with an MIC of 0.5 μg/mL, and this activity is dependent on the presence of SaClpP[1].
ClpP agonist 1 (72 h) exhibits cytotoxicity against HepG2 cells, with an IC50 of 3.10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, 18-20 g, SPF grade)[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:s.c.; daily; 3 consecutive days
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Result:Showed no statistically significant differences in body weight compared to the vehicle group, with no compound-related adverse effects noted.
Reduced lesion size from baseline significantly in a dose-dependent manner.
Decreased MRSA load in skin tissues remarkably compared to the vehicle group, with the 10 mg/kg dose group showing the most pronounced reduction.
Markedly alleviated tissue damage, including reduced epidermal necrosis, dermal thickening, and inflammatory cell infiltration, while preserving normal histological architecture.
Chemical Information
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CAS No. 2761081-10-9
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Molecular Weight 476.44
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Formula C24H21F5N4O
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SMILES
O=C1C2=C(N3CCN=C3N1CC4=CC=C(C=C4)C(F)(F)F)CCN(C2)CC5=CC(F)=CC(F)=C5
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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)