2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial ClpP
  4. 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.

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ClpP agonist 1

ClpP agonist 1 Chemical Structure

CAS No. : 2761081-10-9

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ClpP agonist 1 Related Antibodies

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Description

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[1].

In Vitro

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.

ClpP agonist 1 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-t MRT0-t T1/2 Tmax CL Cmax Bioavailability
Mice[1] 5 mg/kg i.v. 1955.2 ng·h/mL 1.09 h 0.81 h / 2.55 L/h/kg 1982.5 ng/mL /
Mice[1] 10 mg/kg p.o. 1310.5 ng·h/mL 2.29 h 1.92 h 0.75 h 7.30 L/h/kg 432 ng/mL 33.5 %
In Vivo

ClpP agonist 1 (Compound Z1) (2.5-10 mg/kg; s.c.; daily; 3 consecutive days) exhibits significant, dose-dependent therapeutic effects against MRSA skin infection in BALB/c mice, reducing lesion size, bacterial burden, and histopathological tissue damage with a favorable safety profile at tested doses[1].

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

Animal Model: BALB/c (female, 6-8 weeks old, 18-20 g, SPF grade)[1]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: s.c.; daily; 3 consecutive days
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.
Molecular Weight

476.44

Formula

C24H21F5N4O
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ClpP agonist 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:

ClpP agonist 12761081-10-9ClpP agonist1ClpP agonist-1BacterialClpPCaseinolytic protease PMRSA ATCC 33591S. aureus 8325methicillin-resistant staphylococcus aureusmurine skin infection modelBALB/c miceStaphylococcus aureusHepG2 cellsα-caseinmiceStaphylococcus aureus ClpPInhibitorinhibitorinhibit

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