別名

(±)-Ibuprofen - CAS 15687-27-1 - Calbiochem,[(±)-2-(4-Isobutylphenyl)-propionic Acid

一般描述

A nonsteroidal anti-inflammatory drug (NSAID) that acts as a reversible and competitive inhibitor of cyclooxygenase 1 (COX-1) (IC50 = 4.85 μM). Inhibits COX-2 at higher concentrations (IC50 = 223 μM). Blocks aspirin inactivation of COX-1 (EC50 antagonism of 200 μM aspirin = 290 nM). Shown to reduce the total Aβ secretion (Amyloid β40 and 42) in human neuronal cells and offers neuroprotection against glutamate-, nitric oxide-, and superoxide-induced damage. Reported to activate peroxisome proliferator-activated receptors (PPAR) α and γ in both CV-1 and C3H10T1/2 cells (~100 μM-500 μM). A nonsteroidal anti-inflammatory drug (NSAID) that acts as a reversible, competitive, non-selective cyclooxygenase (COX) inhibitor (IC50 = 4.85 μM for purified COX-1 and 223 μM for purified COX-2). Also reported to inhibit COX-1 and COX-2 activity in intact bovine aortic endothelial cells (BAEC) (IC50 = 7 μM for COX-1 and 72.7 μM for COX-2). Potently blocks aspirin inactivation of COX-1 (EC50 antagonism of 200 μM aspirin ~290 nM for ovine COX-1). Decreases the secretion of total Aβ (Amyloid β40&42) by human neuronal cells and offers neuroprotection against glutamate-, nitric oxide- and superoxide-induced damage. Activates peroxisome proliferator activated receptors α and γ in both CV-1 and C3H10T1/2 cells (~100 μM - 500 μM).

生化/生理作用

Cell permeable: no Primary Target
COX-1 Product competes with ATP. Reversible: yes Target IC50: 4.85 μM against COX-1

重懸

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他說明

Asanuma, M., et al. 2001. J. Neurochem.76, 1895.
Blasko, I., et al. 2001. Neurobiol. Dis.8, 1094.
Ouellet, M., et al. 2001. Proc. Natl. Acad. Sci. USA98, 14583.
Casper, D., et al. 2000. Neurosci. Lett.289, 201.
Lambat, Z., et al. 2000. Metab. Brain Dis.15, 249.
Lim, G.P., et al. 2000. J. Neurosci.20, 5709.
Ogawa, O., et al. 2000. Eur. J. Pharmacol.408, 137.
Wyss-Coray, T., and Mucke, L. 2000. Nat. Med.6, 973.
Lehmann, J.M., et al. 1997. J. Biol. Chem.272, 3406.
Boneburg, E.M., et al. 1996. J. Clin. Pharmacol.36, 16S.
Mitchell, J.A., et al. 1994. Proc. Natl. Acad. Sci. USA90, 11693.