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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 | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related PAR Products |
|---|
| ML161
Parmodulin 2 (ML161) is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM. |
| Vorapaxar
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM. |
| Vorapaxar Sulfate
Vorapaxar is a first-in-class, potent and orally-active protease-activated receptor 1 (PAR-1) antagonist that blocks thrombin-mediated platelet activation without interfering with thrombin-mediated fibrin deposition. |
| ML354
ML354 is a potent and selective PAR4 (protease activated receptor-4) antagonist. |
| PAR-4 (1-6) (human)
PAR-4 (1-6) (human) is an N-terminal fragment of protease-activated receptor 4 (PAR4) that acts as a PAR4 agonist. |
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