AZ3451 is a potent PAR2 (protease-activated receptor-2) antagonist with IC50 of 23 nM, which 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.
In vivo, intra-articular injection of AZ3451 can ameliorate the surgery induced cartilage degradation in rat Osteoarthritis (OA) model.
Cell Experiment | |
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Cell lines | chondrocytes |
Preparation 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. |
Concentrations | 10 μM |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | male 8-week-old Sprague-Dawley rats |
Formulation | dissolved in physiological saline |
Dosages | 100 μl (50 μg/ml) |
Administration | intra-articular injection |
Molecular Weight | 571.46 |
Formula | C30H27BrN4O3 |
CAS Number | 2100284-59-9 |
Solubility (25°C) | DMSO ≥ 80 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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