Overview
- Jahangir, A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1632.
Alomone Labs Ro-51 inhibits P2X3 channels expressed in HEK-293 cells.Dose-response curve of P2X3 inhibition by Ro-51 (#R-195). Cells were loaded with Calcium-6 dye, incubated for 5 min with increasing concentrations of Ro-51, and stimulated by 3 µM α,β-MeATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was determined at 4 nM.
- Jahangir, A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1632.
- Serrano, A. et al. (2012) J. Neurosci. 32, 11890.
- Pijacka, W. et al. (2016) Nat Med. 22, 1151.
Ro-51 is a highly potent and selective antagonist of P2X3 and P2X2/3 receptors. It inhibits rat homomeric P2X3 and human heteromeric P2X2/3 and demonstrates IC50 values of 2 and 5 nM respectively1.
Ro-51 has been shown to reduced hyperalgesia and mechanical allodynia in inflammatory and neuropathic pain models1,2. The compound is highly selective for P2X3 and P2X2/3, showing no antagonistic activity at other P2X receptor family members1.
P2X receptors are a family of ion channels gated by ATP. They are widely localized in cell types of almost every origin, including neuronal, muscular, epithelial and immune and have been shown to play a pivotal role in models of various pain conditions3.
Ro-51 (#R-195) is a highly pure, synthetic, and biologically active compound.
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