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Ro 1138452 hydrochloride
Biological Activity for Ro 1138452 hydrochloride
Ro 1138452 hydrochloride is a selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable.
Compound Libraries for Ro 1138452 hydrochloride
Technical Data for Ro 1138452 hydrochloride
|Storage||Desiccate at RT|
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.
Solubility Data for Ro 1138452 hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Ro 1138452 hydrochloride
The following data is based on the product molecular weight 345.87. 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||2.89 mL||14.46 mL||28.91 mL|
|5 mM||0.58 mL||2.89 mL||5.78 mL|
|10 mM||0.29 mL||1.45 mL||2.89 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
Product Datasheets for Ro 1138452 hydrochloride
References for Ro 1138452 hydrochloride
References are publications that support the biological activity of the product.
Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID: 15013022
Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID: 16880763
Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID: 16331286
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Citations for Ro 1138452 hydrochloride
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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.