生物活性
Ketoprofen (Actron) is a non-selective NSAID exhibiting IC50 of 0.5 μM and 2.33 μM for human recombinant COX-1 and COX-2, respectively. It is used for its antipyretic, analgesic, and anti-inflammatory properties by inhibiting cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes reversibly, which decreases production of pro-inflammatory prostaglandin precursors. Based on in vitro IC (50) COX-1:IC (50) COX-2 ratios, robenacoxib was COX-2 selective (ratio=32.2), diclofenac (ratio=3.9) and meloxicam (ratio=2.7) were only weakly COX-2 preferential, and ketoprofen (ratio=0.049) was COX-1 selective.
化学数据
分子量 | 254.28 |
分子式 | C16H14O3 |
CAS号 | 22071-15-4 |
纯度 | 99.11% |
溶解性(25°C) | DMSO 46 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 |
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
以下数据基于产品分子量,对于特殊产品,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 | 3.9327 mL | 19.6634 mL | 39.3267 mL |
5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL |
10 mM | 0.3933 mL | 1.9663 mL | 3.9327 mL |