BGC 20-1531 hydrochloride
High affinity and selective EP4 antagonist (Ki = 3 nM). Exhibits >2500-fold selectivity for EP4 over EP2 and EP3. Also selective over a range of other prostanoid receptors, ion channels, transporters and enzymes. Inhibits PGE2-induced vasodilation of middle cerebral and meningeal arteries in vitro, and carotid blood flow in vivo. Orally bioavailable.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 529. 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||1.89 mL||9.45 mL||18.9 mL|
|5 mM||0.38 mL||1.89 mL||3.78 mL|
|10 mM||0.19 mL||0.95 mL||1.89 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References are publications that support the biological activity of the product.
Sutton et al (2014) From virtual to clinical: The discovery of PGN-1531, a novel antagonist of the prostanoid EP4 receptor. Bioorg.Med.Chem.Lett. 24 2212 PMID: 24703233
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Literature in this Area
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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.