Biological Activity
Potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 6.7) that displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. Stimulates cell proliferation, PI hydrolysis and Ca2+ mobilization in vitro (pEC50 values are 6.7, 5.9 and 6.6 respectively) and exhibits pronociceptive activity in vivo.
Technical Data
| M. Wt | 518.36 |
| Formula | C25H20BrN5O3 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 916170-19-9 |
| PubChem ID | 9589606 |
| InChI Key | UCUHFWIFSHROPY-RWPZCVJISA-N |
| Smiles | O=C2C1=CC=CC=C1C(C(NC(C3=CC=CC=C3)=O)C(N/N=C(C)/C4=CC=CC(Br)=C4)=O)=NN2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.92 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 518.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.93 mL | 9.65 mL | 19.29 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Seitzberg et al (2008) Discovery of potent and selective small-molecule PAR-2 agonists. J.Med.Chem. 51 5490 PMID: 18720984
Gardell et al (2008) Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J.Pharmacol.Exp.Ther. 327 799 PMID: 18768780
Keywords: AC 55541, supplier, Potent, selective, PAR2, agonists, Receptors, Protease-Activated, proteinase-activated, AC55541, Protease-Activated, Receptors, Protease-Activated, Receptors, Tocris Bioscience
