15307-86-5
15307-86-5 结构式
基本信息
奥尔芬
2-[(2,6-二氯苯基)氨基]-苯乙酸
(N-1-(2,6-DICHLOROPHENYL) -2-INDOLIN-2-ONE
Diciofenac
2-[[2,6-Dichlorophenyl] amino] benzeneacetic acid
1-(2,6-DICHLOROPHENYL)-2-INDOLINONE /MEQUITAZINE
1-(2,6-DICHLOROPHENYL)-2-INDOLINONE/INDOLINONE
DICLOFENAC ACID/[2-(2,6-DICHLORO-PHENYLAMINO)-PHENY]-ACETIC ACID
(o-(2,6-dichloroanilino)phenyl)-acetic acid
dichlofenac
[2-(2,6-Dichloroanilino)phenyl]-acetic acid
2-[2-(2,6-Dichlorophenyl)aminophenyl]ethanoic acid
Diclofenac
DICLOFENAC FREE ACID
Rhumalgan
2-(2-(2,6-dichlorophenylamino)phenyl)acetic acid
物理化学性质
常见问题列表
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。
|
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). |