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Submit ReviewGW 627368
Description: Selective EP4 receptor competitive antagonist
Chemical Name: 4-(4-,9-Diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)benzeneacetamide
Purity: ≥98% (HPLC)
Biological Activity
Selective prostanoid EP4 receptor competitive antagonist with additional affinity at TP receptors (pKi values are 7.0 and 6.8 in competition radioligand bioassays). Affinity for all other prostanoid receptors is < 5.3. Inhibits U-46619 induced human platelet aggregation.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries
GW 627368 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 544.62 |
| Formula | C30H28N2O6S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 439288-66-1 |
| PubChem ID | 5312130 |
| InChI Key | XREWXJVMYAXCJV-UHFFFAOYSA-N |
| Smiles | O=C(NS(C5=CC=CC=C5)(=O)=O)CC(C=C4)=CC=C4N3CC2=C(OCC)C1=CC=CC=C1C(OCC)=C2C3=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.46 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 544.62. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.84 mL | 9.18 mL | 18.36 mL |
| 5 mM | 0.37 mL | 1.84 mL | 3.67 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.84 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Wilson et al (2006) GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br.J.Pharmacol. 148 326 PMID: 16604093
Jones and Chan et al (2005) Investigation of the agonist activity of prostacyclin analogues on prostanoid EP4 receptors using GW 627368 and taprostene: evidence for species differences. Prostaglandins Leukot.Essent.Fatty.Acids. 72 289 PMID: 15763441
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Keywords: GW 627368, GW 627368 supplier, GW627368, Prostanoid, receptors, EP4, TP, competitive, antagonists, platelet, aggregation, Receptors, 4668, Tocris Bioscience
1 Citation for GW 627368
Citations are publications that use Tocris products. Selected citations for GW 627368 include:
Edén et al (2015) Tissue factor/factor VIIa signalling promotes cytokine-induced beta cell death and impairs glucose-stimulated Ins secretion from human pancreatic islets. Diabetologia 58 2563 PMID: 26271343
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