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Art. -Nr.: HY-182033

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ClpP agonist 1

ClpP agonist 1 is a Staphylococcus aureus ClpP (SaClpP) agonist with an EC₅₀ of 1.44 μM, K_d 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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CAS. Nr.: 2761081-10-9
Formel: C₂₄H₂₁F₅N₄O
Molecular Weight:476.44

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ClpP agonist 1 Chemical Structure

CAS. Nr.: 2761081-10-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Protokoll (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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. Further protocols information, click here.

Parmacokinetics

Species	Dose	Route	AUC_0-t	MRT_0-t	T_1/2	T_max	CL	C_max	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.

Chemical Information

CAS. Nr. 2761081-10-9
Molecular Weight 476.44
Formel C₂₄H₂₁F₅N₄O
SMILES

O=C1C2=C(N3CCN=C3N1CC4=CC=C(C=C4)C(F)(F)F)CCN(C2)CC5=CC(F)=CC(F)=C5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Protokoll

All Signal Pathway Related

Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Liu Y, et al. Discovery and characterization of Z1: an imipridone-based ClpP agonist with potent anti-staphylococcal activity. Bioorg Chem. 2026;173:109685. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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