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Cat. No.: 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 No.: 2761081-10-9
Formule: C₂₄H₂₁F₅N₄O
Masse moléculaire:476.44

Stockage:

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

ClpP agonist 1 Chemical Structure

CAS No.: 2761081-10-9

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Activité biologique
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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.

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 No. 2761081-10-9
Masse moléculaire 476.44
Formule C₂₄H₂₁F₅N₄O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

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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.

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100 mg

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