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 Information

Prices listed here are the Manufacturer's Suggested European Retail Price. The actual prices quoted by each individual distributor may vary. Please visit the Global Buyer's Guide on the Cayman Chemical (world) website to locate a distributor in your region.

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Size Price Quantity
1 mg €51.00
5 mg €227.00
10 mg €404.00
50 mg €1,764.00
Pricing updated 2010-09-09.
Prices are subject to change without notice.