| Chemical Properties | Back Directory | [Boiling point ]
684.2±55.0 °C(Predicted) | [density ]
1.238±0.06 g/cm3(Predicted) | [solubility ]
DMF: 30 mg/mL; DMSO: 17 mg/mL; Ethanol: 50 mg/mL; PBS (pH 7.2): 3 mg/mL | [form ]
Liquid | [pka]
4.77±0.10(Predicted) | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [Description]
Prostaglandin E2 (PGE2; ) activates four E prostanoid (EP) receptors, EP1-4. 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. CAY10684 is a lactam that acts as a potent EP4 agonist, triggering cAMP signaling with an EC50 value of 0.8 nM. It displays more than 1,000-fold selectivity for EP4 over other EP receptors. | [Uses]
(2R)-2-[(1E)-3-(4''-Chloro-2''-methyl[1,1''-biphenyl]-3-yl)-3-hydroxy-1-propen-1-yl]-5-oxo-1-pyrrolidineheptanoic Acid is an EP4 receptor agonist. | [IC 50]
EP4: 0.8 nM (EC50); EP2: >100000 nM (Ki); EP3: 38000 nM (Ki); EP4: 3.1 nM (Ki) | [References]
[1] YONG S. CHYUN Lawrence G R. Stimulation of bone formation by prostaglandin E2[J]. Prostaglandins, 1984, 27 1: Pages 97-103. DOI: 10.1016/0090-6980(84)90223-5
[2] G HAWCROFT M A H C W S Ko. Prostaglandin E2-EP4 receptor signalling promotes tumorigenic behaviour of HT-29 human colorectal cancer cells[J]. Oncogene, 2006, 26 21: 3006-3019. DOI: 10.1038/sj.onc.1210113
[3] VLADIMIR R BABAEV. Macrophage EP4 deficiency increases apoptosis and suppresses early atherosclerosis.[J]. Cell metabolism, 2008: 492-501. DOI: 10.1016/j.cmet.2008.09.005
[4] TODD R. ELWORTHY et al. et al. Lactams as EP4 Prostanoid Receptor Subtype Selective Agonists. Part 1. 2-Pyrrolidinones — Stereochemical and Lower Side-Chain Optimization.[J]. ChemInform, 2004, 35 34. DOI: 10.1002/chin.200434228 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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