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A. Wako's Unique Products - 1. Inhibitors

a. COX-1-Selective Inhibitor


Wako Catalog No. 205-17381 (10 mg) <for Cellbiology> Keep at -20°C

Cyclooxygenase 1(COX-1) inhibition has been thought to be a major mechanism of gastric damage by nonsteroidal anti-inflammatory drugs (NSAIDs). Dr. Kakuta reported that TFAP [ N-(5-Amino-2-pyridinyl)-4-(trifl uoromethyl)benzamide)], which has a structure clearly different from those of currently available COX-1-selective inhibitors, is a potent COX-1-selective inhibitor (COX-1: IC50 = 0.80 ± 0.05 µM; COX-2: IC50 = 210 ± 10 µM). TFAP causes little gastric damage in rats even at an oral dose of 300 mg/kg, though it has an analgesic effect at as low a dose as 10 mg/kg. The results show that COX-1-selective inhibitors can be analgesic agents without causing gastric damage. Wako has launched TFAP as a novel COX-1-selective inhibitor.

Gastric Ulcer Formation Test using Rat Stomach

Photographs of gastric damage of TFAP and Indomethacin Scale bars indicate 5 mm. White triangles indicate ulcers.
a) Vehicle; b) treated with TFAP (300 mg/kg; p.o.); c) treated with indomethacin (10 mg/kg; p.o.); d) enlarged illustration of part c: While gastric damage was shown from the administration of indomethacin, no damage from TFAP administration.

Analgesic Effect Test

Acetic acid-induced writhing test in mice
Gray and black bars indicate number of writhes at 10 and 30 mg/kg; p.o., respectively. Each value is the average of the total number of writhes ± SEM ( n = 10-11/group). The followings indicate significant differences from the vehicle: (*) p < 0.05; (**) p < 0.01

Chorioallantoic Membrane (CAM) Assay

The angiogenesis activity of TFAP was evaluated by the assay of chick chorioallantoic membrane (CAM). TFAP inhibited CAM angiogenesis at a 300 ng/CAM. TFAP was orally administered at 30 and 300 mg/kg. Data shown are the average of blood vessels/egg ± SEM ( n = 6/group). The following indicates significant difference from the vehicle: (*) p < 0.05

( All data were provided by Dr. Hiroki Kakuta, Division of Pharmaceutical Sciences, Okayama Univ. Graduate School of Medicine, Dentistry and Pharmaceutical Sciences)

Kakuta, H. et al.: Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. Design and in vitro/ in vivo evaluation of a Benzamide-type Cyclooxygenase-1- selective inhibitor, J. Med. Chem., 51, 2400-2411 (2008).
Description Wako Catalog No. (Pkg. Size) Note

<for Cellbiology>
205-17381 (10 mg) Novel Cyclooxigenase-1-Selective Inhibitor
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Wako Product Update Bio-No.3 [ page. 3 ]