双氯芬酸二乙胺

生物活性靶点体外研究体内研究双氯芬酸二乙胺试剂级价格

双氯芬酸二乙胺

CAS号:78213-16-8
英文名:Diclofenac diethylamine
中文名:双氯芬酸二乙胺
CBNumber:CB4113263
分子式:C18H22Cl2N2O2
分子量:369.29
MOL File:78213-16-8.mol

双氯芬酸二乙胺化学性质

熔点 :145-148°C
储存条件 :Inert atmosphere,Room Temperature
溶解度 :DMF: 30 mg/ml; DMSO: 10 mg/ml; Ethanol: 30 mg/ml; PBS (pH 7.2): 2 mg/ml
形态 :A crystalline solid
稳定性 :Hygroscopic
CAS 数据库 :78213-16-8(CAS DataBase Reference)

双氯芬酸二乙胺化学药品说明书

双氯芬酸二乙胺凝胶

双氯芬酸二乙胺性质、用途与生产工艺

生物活性 Diclofenac Diethylamine是一种非类固醇消炎药，用于减轻炎症和某些状况下的止痛药。Diclofenac通过抑制COX1和COX2来抑制前列腺素合成，发挥其功能。

靶点

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 )

体外研究
Diclofenac diethylamine抗炎，退热，和镇痛作用的主要作用机制被认为是通过抑制环氧合酶(COX)，从而抑制前列腺素合成。它通过抑制细菌DNA合成发挥出抑菌活性。COX的抑制也会减少胃上皮细胞中的前列腺素，使其对胃酸的腐蚀更敏感。这也是diclofenac diethylamine的主要副作用。Diclofenac diethylamine阻断COX2-同工酶(大约10倍)，具有低到中度的选择性，因此，diclofenac diethylamine造成的胃肠疾病的发生率比消炎痛和阿司匹林低。

体内研究

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).