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Potent and selective EP3 antagonist (IC50 = 4.6 nM). Inhibits PGE2 facilitation of platelet aggregation in vitro and ex vivo. Displays good plasma and metabolic stability. Does not affect bleeding time in rats. Antiplatelet and antithrombotic.
|Storage||Store at +4°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 592.32. 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||1.69 mL||8.44 mL||16.88 mL|
|5 mM||0.34 mL||1.69 mL||3.38 mL|
|10 mM||0.17 mL||0.84 mL||1.69 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
References are publications that support the biological activity of the product.
Markovič et al (2017) Structural features of subtype-selective EP receptor modulators. Drug Discov.Today. 22 57 PMID: 27506873
Singh et al (2009) Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem.Biol. 4 115 PMID: 19193156
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Keywords: DG 041, DG 041 supplier, DG041, potent, selective, EP3, antagonists, Receptors, Prostanoid, prostaglandins, prostacyclins, eicosanoids, 6240, 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.