Prostaglandin E₂ (PGE₂; Item No. 14010) activates four E prostanoid (EP) receptors, EP_1-4. EP₄ is a G protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.^1,2,3 CAY10684 is a lactam that acts as a potent EP₄ agonist, triggering cAMP signaling with an EC₅₀ value of 0.8 nM.⁴ It displays more than 1,000-fold selectivity for EP₄ over other EP receptors.⁴

≥98%

Store at -20℃

1.Li, M.,Thompson, D.D. and Paralkar, V.M. Prostaglandin E₂ receptors in bone formation. International Orthopaedics 31, 767-772 (2007).

2.Hawcroft, G.,Ko, C.W.S. and Hull, M.A. Prostaglandin E₂-EP₄ receptor signalling promotes tumorigenic behaviour of HT-29 human colorectal cancer cells. Oncogene 26, 3006-3019 (2007).

3.Babaev, V.R.,Chew, J.D.,Ding, L., et al. Macrophage EP₄ deficiency increases apoptosis and suppresses early atherosclerosis. Cell Metabolism 8, 492-501 (2008).

4.Elworthy, T.R.,Kertesz, D.J.,Kim, W., et al. Lactams as EP₄ prostanoid receptor subtype selective agonists. Part 1: 2-Pyrrolidinones-sterochemical and lower side-chain optimization. Bioorganic & Medicinal Chemistry Letters 14, 1655-1659 (2004).