Chemical Name: (±)-(3R*,4S*)-2-Oxo-4-phenyl-3-pyrollidinecarboxylic acid 2-[1-(3-bromophenyl)ethylidene]hydrazide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation. Stimulates PI hydrolysis, Ca2+ mobilization and cellular proliferation in vitro (pEC50 values are 6.9, 7.0 and 7.5 respectively).
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Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
40.03
100
Preparing Stock Solutions
The following data is based on the product molecular weight 400.27. 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
2.5 mL
12.49 mL
24.98 mL
5 mM
0.5 mL
2.5 mL
5 mL
10 mM
0.25 mL
1.25 mL
2.5 mL
50 mM
0.05 mL
0.25 mL
0.5 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Gardellet al (2008) Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J.Pharmacol.Exp.Ther. 327 799 PMID: 18768780
Seitzberget al (2008) Discovery of potent and selective small-molecule PAR-2 agonists. J.Med.Chem. 51 5490 PMID: 18720984