货号 | 10010088-1mg |
描述 | 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 |
供应商 | Cayman |
应用文献 | |
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. Journal of Immunology 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. The Journal of Biological Chemisty 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. Journal of Immunology 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. Journal of Medicinal Chemistry 50, 2176-2184 (2007). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 311.1 |
分子式 | C12H7BrO3S |
CAS号 | 938069-71-7 |
稳定性 | ≥ 2 years |
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