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Potent, dual P2X3 and P2X2/3 antagonist (IC50 values are 2 and 5 nM for rP2X3 and hP2X2/3 respectively). Selective for P2X3 and P2X2/3 over other P2X receptors (IC50 values are > 10 μM for P2X1, P2X2, P2X4, P2X5, and P2X7). Cell permeable.
|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 474.29. 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||2.11 mL||10.54 mL||21.08 mL|
|5 mM||0.42 mL||2.11 mL||4.22 mL|
|10 mM||0.21 mL||1.05 mL||2.11 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Jahangir et al (2009) Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X3/P2X2/3 antagonist for the treatment of pain. Bioorg.Med.Chem.Lett. 19 1632 PMID: 19231178
Syed and Kennedy (2012) Pharmacology of P2X receptors WIREs.Membr.Transp.Signal. 1 16
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Keywords: Ro 51, Ro 51 supplier, Ro51, Potent, selective, P2X3, P2X2/3, P2X, purinergic, receptors, antagonists, purinoceptors, Receptors, 4391, Tocris Bioscience
1 Citation for Ro 51
Citations are publications that use Tocris products. Selected citations for Ro 51 include:
Lu et al (2019) Adenosine triphosphate is co-secreted with glucagon-like peptide-1 to modulate intestinal enterocytes and afferent neurons. Nat.Commun. 10 1029 PMID: 30833673
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.