357605-73-3
Chemical Structure
ONO-AE2-227
- CAS No.: 357605-73-3
- Formula:C27H23NO3
- Molecular Weight:409.49
IUPAC Name: 2-(2-(2-(naphthalen-1-yl)propanamido)benzyl)benzoic acid
InChIKey: BLJLWFKNTKAUDA-UHFFFAOYSA-N
SMILES: O=C(O)C=1C=CC=CC1CC=2C=CC=CC2NC(=O)C(C3=CC=CC=4C=CC=CC43)C
Biological Activity: ONO-AE2-227 is an orally active EP4 receptor antagonist. ONO-AE2-227 blocks PGE2-mediated EP4 signaling by competitively antagonizing PGE2-induced cAMP elevation, and binds to EP4/EP3 with mouse Ki values of 2.7/21 nM. ONO-AE2-227 reduces aberrant crypt foci and intestinal polyp development, and inhibits intestinal polyp formation. ONO-AE2-227 enhances LPS-induced TNF-alpha release from human alveolar macrophages by blocking endogenous PGE2, blocks PGE2-induced ICAM-1 expression and leukocyte-endothelial adhesion, and attenuates PGE2-induced monocyte adhesion to brain endothelial cells. ONO-AE2-227 can be used for research on colon cancer[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
ONO-AE2-227 | ONO-AE2-227 is an orally active EP4 receptor antagonist. ONO-AE2-227 blocks PGE2-mediated EP4 signaling by competitively antagonizing PGE2-induced cAMP elevation, and binds to EP4/EP3 with mouse Ki values of 2.7/21 nM. ONO-AE2-227 reduces aberrant crypt foci and intestinal polyp development, and inhibits intestinal polyp formation. ONO-AE2-227 enhances LPS-induced TNF-alpha release from human alveolar macrophages by blocking endogenous PGE2, blocks PGE2-induced ICAM-1 expression and leukocyte-endothelial adhesion, and attenuates PGE2-induced monocyte adhesion to brain endothelial cells. ONO-AE2-227 can be used for research on colon cancer. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Jones RL, et al. Prostanoid receptor antagonists: development strategies and therapeutic applications. British journal of pharmacology. 2009 Sep;158(1):104-45.
- [2]. Mutoh M, et al. Involvement of prostaglandin E receptor subtype EP(4) in colon carcinogenesis. Cancer Res. 2002 Jan 1;62(1):28-32.
- [3]. Ratcliffe MJ, et al. Activation of E-prostanoid4 and E-prostanoid2 receptors inhibits TNF-alpha release from human alveolar macrophages. The European respiratory journal. 2007 May;29(5):986-94.
- [4]. Park TY, et al. Prostaglandin E₂-induced intercellular adhesion molecule-1 expression is mediated by cAMP/Epac signalling modules in bEnd.3 brain endothelial cells. British journal of pharmacology. 2013 Jun;169(3):604-18.
