There are only two cyclooxygenases (COX-1 and COX-2) in man, and there are no fewer than 6 lipoxygenases, one of which has been unequivocally linked to human disease, viz., 5-lipoxygenase (5-LO). Human 5-lipoxygenase (5-LO) is the key enzyme of leukotriene biosynthesis, mostly expressed in leukocytes and thus a crucial component of the innate immune system.

Firstly, the Metabolism of arachidonic acid along two major metabolic pathways, the cyclooxygenase (COX) and lipoxygenase (LO) pathways. It leads to several families of lipid mediators, including prostaglandins, thromboxane, leukotrienes, and lipoxins. Secondly, these compounds, collectively known as eicosanoids, possess potent biological activities and are involved in the maintenance of normal hemostasis, regulation of blood pressure, renal function, and reproduction as well as host defense. Furthermore, when formed in excess under pathological conditions, these molecules can elicit pain, fever, and inflammation and play roles in many acute and chronic endemic diseases.

BW 755C is a 5-LO inhibitor for inflammation research.

In vitro, BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits COX with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively.

In vivo, BW 755C (0.03-10 mg/rat; s.c.; once) inhibits the ovulation rate and ovarian levels of 5-HETE and 12-HETE in rats.


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