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CAY10526 Exclusive

Cayman Chemical Item Number 10010088

(CAS 938069-71-7)

CAY10526 (CAS 938069-71-7)

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Description

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).

Formal Name 4-​(benzo[b]thiophen-​2-​yl)-​3-​bromo-​5-​hydroxydihydrofuran-​2(3H)-​one
CAS Number 938069-71-7
Molecular Formula C12H7BrO3S
Formula Weight 311.1
Formulation A crystalline solid
Purity ≥98%
λmax 215, 332 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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OC1OC(=O)​C(Br)​C1c1cc2ccccc2s1

Background Reading

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).

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).

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).

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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CAY10526 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $43.00 $0.00
5 mg $194.00 $0.00
10 mg $344.00 $0.00
50 mg $1,505.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-25. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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