AZ3451

Catalog No.S9744

For research use only.

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.

AZ3451 Chemical Structure

CAS No. 2100284-59-9

Purity & Quality Control

Choose Selective PAR Inhibitors

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 (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[2]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 571.46
Formula

C30H27BrN4O3

CAS No. 2100284-59-9
Storage 3 years -20°C powder
2 years -80°C in solvent

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