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Selective EP1 prostanoid receptor antagonist (Ki values are 1.3, 11.2, 17.5, 61.1, > 100, > 100, > 100, >100 and > 100 μM for EP1, TP, EP3, EP2, EP4, FP and DP receptors respectively). Attenuates PGE2-induced neuronal cell death in vitro and slows tumor growth in vivo.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at -20°C|
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|
Preparing Stock Solutions
The following data is based on the product molecular weight 459.33. 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||2.18 mL||10.89 mL||21.77 mL|
|5 mM||0.44 mL||2.18 mL||4.35 mL|
|10 mM||0.22 mL||1.09 mL||2.18 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Abramovitz et al (2000) The utilization of recombinant prostanoid receptors determine the affinities and selectivities of prostaglandins and related analogs. Biochim.Biophys.Acta 1483 285 PMID: 10634944
Saleem et al (2007) Effect of EP1 receptor on cerebral blood flow in the middle cerebral artery occlusion model of stroke in mice. J.Neurosci.Res. 85 2433 PMID: 17600836
Matsuo et al (2004) Inhibition of human glioma cell growth by a PHS-2 inhibitor, NS398, and a prostaglandin E receptor subtype EP1-selective antagonist. J.Neurochem. 66 285
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Keywords: SC 51089, SC 51089 supplier, SC51089, selective, EP1, receptors, antagonists, prostanoids, PGE2, prostaglandins, prostacyclins, eicosanoids, Pfizer, Prostanoid, Receptors, 3758, Tocris Bioscience
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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.