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Submit ReviewGW 627368 is a 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.
Sold for research purposes under agreement from GlaxoSmithKline.
GW 627368 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 54.46 | 100 |
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 |
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
If you know of a relevant reference for GW 627368, please let us know.
Keywords: GW 627368, GW 627368 supplier, GW627368, Prostanoid, receptors, EP4, TP, competitive, antagonists, platelet, aggregation, Receptors, 4668, Tocris Bioscience
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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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.