简介: Diclofenac 是一种有效的,非选择性的抗炎剂,为COX的抑制剂,在 CHO 细胞中,对人 COX-1 和 COX-2 的IC50值分别为 4 nM,1.3 nM;Diclofenac 同时对绵羊 COX-1 和 COX-2 的IC50值分别为 5.1 μM,0.84 μM。
中文名:双氯芬酸
物理性状及指标:
外观:……………………Almost white powder
溶解性:…………………Ethanol : ≥ 30mg/ml
含量:……………………≥99%,BR
储存温度:常温,避光防潮密闭干燥
生物活性(仅来自于公开文献)
描述
|
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as aCOXinhibitor, withIC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively. | |||
IC50& Target |
Human COX-2 | Human COX-1 | Ovine COX-2 | Ovine COX-1 |
1.3 nM (IC50, in CHO cells) | 4 nM (IC50, in CHO cells) | 0.84 μM (IC50) | 5.1 μM (IC50) | |
体外 |
Diclofenac is a potent COX inhibitor, with IC50s of 4 nM and 1.3 nM for human COX-1 and COX-2 in the CHO cells, respectively. Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC50of 7 ± 3 nM. Diclofenac sodium exihibits inhibition on COX-1 and COX-2 enzyme with IC50s of 5.1 and 0.84 μM, respectively. | |||
体内 |
Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal51Cr 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) shows anti-inflammatory activity in mice. Diclofenac (10 mg/kg) decreases oxidized low-densitylipoprotein (Ox-LDL), but shows no effects on the kinetics parameters of catalase and glutathione peroxidase via intramuscularly injection into rats. |
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储液配置及储存:按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-55°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃1-3月;-80℃ 3-6月。
浓度/体积(乙醇)/质量 |
1 mg |
5 mg |
10 mg |
1 mM |
3.3767 mL |
16.8833 mL |
33.7667 mL |
5 mM |
0.6753 mL |
3.3767 mL |
6.7533 mL |
10 mM |
0.3377 mL |
1.6883 mL |
3.3767 mL |
【注意】
●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。
●部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,以上数据仅供参考交流研究之用。
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