生物活性
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.
化学数据
| 分子量 | 571.46 |
| 分子式 | C30H27BrN4O3 |
| CAS号 | 2100284-59-9 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO ≥ 80 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | chondrocytes |
| 方法 | 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. |
| 浓度 | 10 μM |
| 处理时间 | 48 h |
| 动物实验 |
|---|
| 动物模型 | male 8-week-old Sprague-Dawley rats |
| 配制 | dissolved in physiological saline |
| 剂量 | 100 μl (50 μg/ml) |
| 给药处理 | intra-articular injection |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于半岛bd体育手机客户端
分子量，对于特殊半岛bd体育手机客户端
，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7499 mL | 8.7495 mL | 17.499 mL |
| 5 mM | 0.35 mL | 1.7499 mL | 3.4998 mL |
| 10 mM | 0.175 mL | 0.875 mL | 1.7499 mL |
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