CAS:15307-86-5Diclofenac

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Diclofenac is a non-selective COX inhibitor with IC50 of 60 and 220 nM for ovine COX-1 and -2, respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

15307-86-5

储存条件

分子式

C14H11Cl2NO2

运输

蓝冰

分子量

296.15

别名

溶解度

DMSO	59.0 mg/mL (199.2 mM)

动物实验配方

生物活性

靶点 COX2

IC50:220nM COX1

IC50:60nM
描述Diclofenac 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. Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50 of 7±3 nM. Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51Cr 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^[3]. Treatment with diclofenac (10 microM) for 2 days induced the death of NSCs in a concentration-dependent manner. Diclofenac also inhibited the proliferation of NSCs and their differentiation into neurons. Treatment with diclofenac resulted in nuclear condensation (a morphological change due to apoptosis of NSCs) 24hr after the treatment and activated caspase-3 after 6 hr, indicating that diclofenac may cause apoptosis of neuronal cells via activation of the caspase cascade^[4].

靶点	Description	IC50
COX2		IC50:220nM
COX1		IC50:60nM