Cayman Chemical | CAY10526

10010088 CAY10526

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• See more Inhibitors; Inflammation; Pain

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Prostaglandin E₂ (PGE₂) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE₂ during inflammation can be accounted for by increased expression of both cyclooxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1).^1,2,3 CAY10526 is an inhibitor of PGE₂ production through the selective modulation of mPGES-1 expression. It dose-dependently inhibits PGE₂ production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC₅₀ value of 1.8 µM without any effect on COX-2 expression.⁴

1 Claveau, D., Sirinyan, M., Guay, J., et al. Microsomal prostaglandin E synthase-1 is a major terminal synthase that is selectively up-regulated during cyclooxygenase-2-dependent prostaglandin E₂ production in the rat adjuvant-induced arthritis model. J Immunol 170 4738-4744 (2003).

2 Guay, J., Bateman, K., Gordon, R., et al. Carrageenan-induced paw edema in rat elicits a predominant prostaglandin E₂ (PGE₂) response in the central nervous system associated with the induction of microsomal PGE₂ synthase-1. J Biol Chem 279(23) 24866-24872 (2004).

3 Stichtenoth, D.O., Thorén, S., Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. J Immunol 167 469-474 (2001).

4 Guerrero, M.D., Aquino, M., Bruno, I., et al. Synthesis and pharmacological evaluation of a selected library of new potential anti-inflammatory agents bearing the γ-hydroxybutenolide scaffold: a new class of inhibitors of prostanoid production through the selective modulation of microsomal prostaglandin E synthase-1 expression. J Med Chem 50 2176-2184 (2007).

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Pricing updated 2010-03-16.
Prices are subject to change without notice.

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