CAS |
15307-86-5 |
Chinese Name |
双氯芬酸 |
English Name |
Diclofenac Acid |
Synonyms |
双氯芬酸;奥尔芬;氯化苄乙氧胺;海明1622; |
Molecular Formula |
C14H11Cl2NO2 |
Molecular Weight |
296.15 |
Solubility |
Soluble in DMSO |
Purity |
≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 239-348-5 |
MDL |
MFCD00451393 |
SMILES |
O=C(O)CC1=CC=CC=C1NC2=C(Cl)C=CC=C2Cl |
InChIKey |
DCOPUUMXTXDBNB-UHFFFAOYSA-N |
InChI |
InChI=1S/C14H11Cl2NO2/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19/h1-7,17H,8H2,(H,18,19) |
PubChem CID |
3033 |
Target Point |
COX |
Passage |
Immunology & Inflammation |
Background |
Diclofenac Acid is a potent, non-selective anti-inflammatory agent that is a COX inhibitor. The mechanism of action is to selectively cut off the action link of cyclooxygenase in the arachidonic acid metabolism series and block the synthesis pathway of prostaglandin E2 (PGE2). |
Biological Activity |
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。[1-3] |
In Vitro |
双氯芬酸是一种有效的COX抑制剂,CHO细胞中人COX-1和COX-2的IC50分别为4 nM和1.3 nM。双氯芬酸有效阻断UX37细胞微粒体中COX-1介导的前列腺素产生,IC50为7±3 nM [1]。双氯芬酸钠表现出对COX-1和COX-2酶的抑制作用,IC50分别为5.1和0.84μM[2]。 |
In Vivo |
双氯芬酸(3mg / kg,bid,5天)显着增加大鼠粪便51Cr排泄,并且在施用1mg / kg每天两次,持续4天后,在松鼠猴中也观察到这种效果[1]。双氯芬酸(10mg / kg)在小鼠中显示出抗炎活性[2]。双氯芬酸(10 mg / kg)可降低氧化低密度脂蛋白(Ox-LDL),但通过肌内注射大鼠对过氧化氢酶和谷胱甘肽过氧化物酶的动力学参数没有影响[3]。 |
Animal Experiment |
大鼠[1]雄性Sprague-Dawley大鼠(150±200g)口服给予双氯芬酸一次(急性给药)或每天两次,持续5天(慢性给药)。在第4天早晨剂量后1小时获得血浆样品,用于测量双氯芬酸浓度。在第5天给予最后一次剂量后,立即通过尾静脉向大鼠注射来自供体大鼠的0.5mL 51Cr标记的红细胞,其与51铬酸钠一起孵育。将大鼠单独置于代谢笼中,随意食物和水。收集粪便48小时,51Cr粪便排泄量计算为总注射剂量的百分比(每只动物20mCi)[1]。松鼠猴[1]松鼠猴(Saimiri sciureus; 0.8±1.4 kg)口服双氯芬酸,每日两次,持续1±5天。给予最后一剂后1小时,通过隐静脉注射51CrCl3的无菌盐水(1mL / kg,每只动物4±5mCi),并获得血浆样品用于测量双氯芬酸浓度。然后将猴子单独圈养在代谢笼中。收集粪便24小时,51Cr粪便排泄量计算为总注射剂量的百分比[1]。 |
Data Literature Source |
[1]. Riendeau D,et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17. [2]. Labib MB,et al. Design,synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory,analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80. [3]. Curcelli EC,et al. Beneficial effects of diclofenac therapy on serum lipids,oxidized low-density lipoprotein and antioxidant defenses in rats. Life Sci. 2008 Apr 9;82(15-16):892-8. |
Unit |
Bottle |
Specification |
500mg 1g |