Overview
Lyophilized Powder yes
Source Synthetic
MW: 474.29
Purity: >98% (HPLC)
Effective concentration 0.2 nM – 0.2 µM.
Structure
Chemical name 2-[[4-amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,3-diol.
Molecular formula C17H23IN4O4.
CAS No.: 1050670-85-3
PubChem CID 24883277
Activity Ro-51 is a highly potent and selective antagonist of P2X3 and P2X2/3 receptors. It has been shown to inhibit rat homomeric P2X3 and human heteromeric P2X2/3 receptors with pIC50 values of 8.7 and 8.3, respectively, whilst exhibiting no antagonistic activity at other P2X receptor family members at up to 10 µM1.
References-Activity
- Jahangir, A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1632.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at +4°C for several weeks. For longer periods, it should be stored at -20°C.
Solubility Up to 100 mM in DMSO or Ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions -20°C.
Our bioassay
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.
Scientific background
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.
Target P2X3 receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
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