Biological Activity
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.
Technical Data
| M. Wt | 474.29 |
| Formula | C17H23IN4O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1050670-85-3 |
| PubChem ID | 24883277 |
| InChI Key | PAYROHWFGZADBR-UHFFFAOYSA-N |
| Smiles | NC1=NC(NC(CO)CO)=NC=C1OC2=C(C(C)C)C=C(OC)C(I)=C2 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.43 | 100 | |
| ethanol | 47.43 | 100 |
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 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 | 2.11 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 PMID:
Keywords: Ro 51, supplier, Ro51, Potent, selective, P2X3, P2X2/3, P2X, purinergic, receptors, antagonists, purinoceptors, P2X, Receptors, P2X, Receptors, Tocris Bioscience
