For research use only.
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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|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.|
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.
Intra-articular injection of AZ3451 can ameliorate the surgery induced cartilage degradation in rat Osteoarthritis (OA) model.
|In vitro||DMSO||100 mg/mL (174.99 mM)|
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|% DMSO % % Tween 80 % ddH2O|
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