| 中文名称 | 双氯芬酸 |
| 英文名称 | 1-(2,6-Dichlorophenyl)-2-indolinone |
| CAS号 | 15307-86-5 |
| 分子式 | C14H11Cl2NO2 |
| 分子量 | 296.15 |
| EINECS号 | 239-348-5 |
| 熔点 | 156-158° |
| 沸点 | 412.0±45.0 °C(Predicted) |
| 密度 | 1.431±0.06 g/cm3(Predicted) |
| 溶解度 | 溶于甲醇 |
| 形态 | 粉末晶体 |
| 酸度系数(pKa) | pKa 4 (Uncertain) |
| 颜色 | 白色到近乎白色 |
| 水溶解性 | 1.278mg/L(30 ºC) |
| 默克索引编号 | 14,3081 |
| 危险品运输编号 | 3249 |
| RTECS号 | AG6310000 |
| 海关编码 | 2922.49.2600 |
| 危险等级 | 6.1(b) |
| 包装类别 | III |
| 毒害物质数据 | 15307-86-5(Hazardous Substances Data) |
双氯芬酸的作用机理为抑制环氧化酶活性，从而阻断花生四烯酸向前列腺素的转化生成，因前列腺素为引起疼痛、发烧及发炎等之现象的主要因子。
双氯芬酸为白色结晶性粉末，无臭，易溶于丙酮，溶于甲，乙醇，微溶于水。双氯芬酸具有显著的抗风湿，消炎，止痛和解热作用，其抗炎作用比阿司匹林强26—50倍，能很好的解除关节疼能，消肿，改善其活动，同时具有良好的耐受性。Diclofenac acid是一种非类固醇的消炎药，具有止痛、消炎和退热活性，在治疗多种急性和慢性疼痛、炎症反应中有效。它能抑制cyclooxygenase-1 (COX-1)和cyclooxygenase-2 (COX-2)，具有相近的效力。|
Human COX-2 1.3 nM (IC 50 , in CHO cells) |
Human COX-1 4 nM (IC 50 , in CHO cells) |
Ovine COX-2 0.84 μM (IC 50 ) |
Ovine COX-1 5.1 μM (IC 50 ) |
Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC
50
of 7±3 nM.
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner.
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3.
Cell Viability Assay
| Cell Line: | Neural stem cells (NSCs) |
| Concentration: | 1, 3, 10, 30, 60 μM |
| Incubation Time: | 1 day |
| Result: | Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM. |
Western Blot Analysis
| Cell Line: | Neural stem cells (NSCs) |
| Concentration: | 10, 30 or 60 μM |
| Incubation Time: | 6 hours |
| Result: | The activation of caspase-3 was increased in a concentration-dependent manner. |
Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal
51
Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days.
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats.
| Animal Model: | Male Sprague-Dawley rats (150±200 g) |
| Dosage: | 3 mg/kg |
| Administration: | Oral administration, b.i.d., for 5 days |
| Result: | Resulted in a significant increase in faecal 51 Cr excretion. |
| Animal Model: | Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model |
| Dosage: | 10 mg/kg |
| Administration: | Administered via oral route just prior to induction of inflammation |
| Result: | Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h). |
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苯乙酸
