Description: High affinity and selective EP2 receptor antagonist
Chemical Name: (2E)-N-[2-(2-Methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
High affinity and selective EP2 receptor antagonist (KB values are 2.4 and 34.5 nM for EP2 and DP1 receptors respectively). Exhibits >500-fold selectivity for EP2 over other prostanoid receptors. Inhibits butaprost-induced proinflammatory cytokine production, cell proliferation and invasion of PC-3 cells in vitro.
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
39.45
100
ethanol
7.89
20
Preparing Stock Solutions
The following data is based on the product molecular weight 394.46. 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
2.54 mL
12.68 mL
25.35 mL
5 mM
0.51 mL
2.54 mL
5.07 mL
10 mM
0.25 mL
1.27 mL
2.54 mL
50 mM
0.05 mL
0.25 mL
0.51 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.
Jiang and Dingledine
(2013) Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation. J.Pharmacol.Exp.Ther. 344 360 PMID: 23192657
Quanet al (2013) EP2 receptor signaling pathways regulate classical activation of microglia. J.Biol.Chem. 288 9293 PMID: 23404506