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AC 264613
- Soluble in DMSO
- MF: C19H18BrN3O2
- MW: 400.27
Description
AC 264613 is a potent, selective and metabolically stable protease-activated receptor 2 (PAR2, F2RL1) agonist with a reported pEC50 value of 6.7. It activates PAR2 signaling and has been reported to modulate inflammatory transcriptional responses in macrophage models.
PAR2 is a G protein-coupled receptor activated by proteolytic cleavage and involved in inflammation, epithelial barrier biology, pain signaling and innate immune responses. AC 264613 is useful for studying PAR2-driven calcium, MAPK and inflammatory signaling without relying on protease activation.
Key Features
- Selective PAR2 agonist
- Reported pEC50: 6.7
- Metabolically stable small-molecule PAR2 activator
- Modulates PAR2-dependent inflammatory signaling
Applications
- PAR2 receptor pharmacology
- Inflammation and innate-immunity studies
- GPCR calcium and MAPK signaling assays
- Macrophage and epithelial response models
More Information
| Parent CAS No. | 1051487-82-1 |
|---|---|
| Chemical Name | N'-(1-(3-Bromophenyl)ethylidene)-2-oxo-4-phenylpyrrolidine-3-carbohydrazide |
| SMILES | C1C=CC=C(C2C(C(=O)N/N=C(C)/C3C=C(Br)C=CC=3)C(=O)NC2)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C19H18BrN3O2/c1-12(14-8-5-9-15(20)10-14)22-23-19(25)17-16(11-21-18(17)24)13-6-3-2-4-7-13/h2-10,16-17H,11H2,1H3,(H,21,24)(H,23,25)/b22-12+ |
| InChiKey | RQKXQCSEZPQBNZ-WSDLNYQXSA-N |
| CID | 11961320 |
| Short Description | PAR2 agonist |
References
- JG Seitzberg et al. Discovery of potent and selective small-molecule PAR-2 agonists. J Med Chem. 2008 Sep 25;51(18):5490-3.
- LR Gardell et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808.
- R Yamaguchi et al. A protease-activated receptor 2 agonist (AC-264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages: Role of p53. Cell Biol Int. 2016 Jun;40(6):629-41.
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