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编 号:F181014
分子式:C14H10Cl2NNaO2
分子量:318.13
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500mg
280
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5g
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生物活性:
Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

体内研究:
Diclofenac Sodium (3 mg/kg,bid,持续 5 天) 显著增加大鼠粪便51 Cr 排泄,并且在给予 1 mg/kg 每天两次持续 4 天后,在松鼠猴中也观察到这种效果。 Diclofenac Sodium (10 mg/kg;在诱导炎症之前通过口服途径给药) 在 Wistar 大鼠体内显示出抗炎活性。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 51Cr 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).

体外研究:
Diclofenac 有效阻断 COX-1 介导的 U937 细胞微粒体产生前列腺素,IC50 为 7±3 nM。 Diclofenac Sodium (1-60 μM;1 天) 以浓度依赖性方式诱导神经干细胞 (NSCs) 死亡。 Diclofenac Sodium (10-60 μM;6 小时) 增加裂解 (激活) caspase-3 的表达。
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