生物活性
Firocoxib is a coxib exhibiting high selectivity to inhibit COX-2. In vitro canine whole blood assays have demonstrated Firocoxib to be 350–430-fold more selective for COX-2 than for COX-1. COX-1 is constitutively expressed and enzymatically active in a variety of sites, including the stomach, intestine, kidneys, and platelets. COX-1 is the isoform largely responsible for the physiologic functions of eicosanoids, including gastric mucosal protection, renal blood flow, and vascular hemostasis. COX-2 expression is primarily induced by mediators such as serum growth factors, cytokines, and mitogens. COX-2 is primarily responsible for the synthesis of eicosanoids associated with inflammation.
化学数据
| 分子量 | 336.4 |
| 分子式 | C17H20O5S |
| CAS号 | 189954-96-9 |
| 纯度 | 100.00% |
| 溶解性（25°C） | DMSO ≥ 45 mg/mL |
| 储存和运输条件 | -20°C, sealed, protect from light
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 | isolated peripheral blood mononuclear cells |
| 方法 | Peripheral blood mononuclear cells were isolated by density gradient centrifugation and incubated at 37°C with medium alone, firocoxib (100 ng/mL), LPS (1 ng/mL or 1 μg/mL), or combinations of firocoxib and both LPS concentrations. After 4 hours, supernatants were collected and tested for prostaglandin E2 (PGE2) concentration with an enzyme inhibition assay, and gene expression in cell lysates was measured with PCR assays. |
| 浓度 | 100 ng/mL |
| 处理时间 | 4h |
| 动物实验 |
|---|
| 动物模型 | Mouse Model of Incisional Pain by objective measurement of mechanical allodynia and thermal hyperalgesia using von Frey and Hargreaves equipment |
| 配制 | diluted in sterile 0.9% physiologic saline |
| 剂量 | 10 or 20 mg/kg |
| 给药处理 | intraperitoneally |
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 | 2.9727 mL | 14.8633 mL | 29.7265 mL |
| 5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL |
| 10 mM | 0.2973 mL | 1.4863 mL | 2.9727 mL |
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