Potent dual antagonist of TP/DP2 (CRTH2) prostanoid receptors (Ki values are 4.3, 4.5 and > 10000 nM for hDP2, hTP and hDP1 receptors respectively). Suppresses PGD2-induced migration of human eosinophils (IC50 = 170 nM).
|Storage||Desiccate at -20°C|
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 416.47. 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||2.4 mL||12.01 mL||24.01 mL|
|5 mM||0.48 mL||2.4 mL||4.8 mL|
|10 mM||0.24 mL||1.2 mL||2.4 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the biological activity of the product.
Sundstrom et al (2003) Interactions among three classes of mediators explain antigen-induced bronchoconstriction in the isolated perfused and ventilated guinea pig lung. J.Pharmacol.Exp.Ther. 307 408 PMID: 12954791
Ishizuka et al (2004) Ramatroban (BAY u3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor. Cardiovasc.Drug Rev. 22 71 PMID: 15179446
Ulven and Kostenis (2005) Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J.Med.Chem. 48 897 PMID: 15715457
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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.