AZ3451

For research use only.

Catalog No.S9744

AZ3451 Chemical Structure

CAS No. 2100284-59-9

AZ3451 is a potent antagonist of protease-activated receptor 2 (PAR2) that binds to a remote allosteric site outside the helical bundle with IC50 of 23 nM.

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Biological Activity

Description AZ3451 is a potent antagonist of protease-activated receptor 2 (PAR2) that binds to a remote allosteric site outside the helical bundle with IC50 of 23 nM.
Targets
PAR2 [1]
(Cell-free assay)
23 nM
In vitro

AZ3451 is a PAR2 antagonist that plays a part in inflammation response, apoptosis, autophagy and cellular senescence during Osteoarthritis (OA). AZ3451 prevents the IL-1β-induced inflammation response, cartilage degradation and premature senescence in chondrocytes. AZ3451 attenuates chondrocytes apoptosis by activating autophagy in vitro. The P38/MAPK, NF-κB and PI3K/AKT/mTOR pathways are involved in the protective effect of AZ3451.[2]

In vivo

Intra-articular injection of AZ3451 can ameliorate the surgery induced cartilage degradation in rat Osteoarthritis (OA) model.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: chondrocytes
  • Concentrations: 10 μM
  • Incubation Time: 48 h
  • Method:

    Primary rat chondrocytes are derived from the knee joint cartilage tissue of 1-week-old Sprague–Dawley rats. Cartilage pieces are sequential digested with 0.2% trypsin and 0.25% collagenase II dissolved in Dulbecco’s Modified Eagle Medium (DMEM) culture medium. The released chondrocytes are collected and cultured in DMEM supplemented with 10% fetal bovine serum (FBS), 100 units/ml penicillin and 100 μg/ml streptomycin. Up to approximately 80% confluences, cells are treated with 10 μM AZ3451 in the presence or absence of 10 ng/mL IL-1β. Passages 1–3 chondrocytes are used in our experiment to avoid the phenotype loss.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: male 8-week-old Sprague–Dawley rats
  • Dosages: 100 μl (50 μg/ml)
  • Administration: intra-articular injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (174.99 mM)
Water Insoluble
Ethanol '100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 571.46
Formula

C30H27BrN4O3

CAS No. 2100284-59-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID