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.
体外研究
Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 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.
体内研究
Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 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 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).
分子式
C14H10Cl2NNaO2
分子量
318.13
CAS号
15307-79-6
中文名称
双氯芬酸钠
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
H2O : 10 mg/mL (31.43 mM; ultrasonic and warming and heat to 60°C)