| Bioactivity | Ro-51 is a potent and selective dual P2X3/P2X2/3 antagonist, with IC50 of 2 nM and 5 nM for P2X3 and P2X2/3, respectively. Ro-51 can be used for the research for pain[1][2]. |
| Target | IC50: 2 nM (P2X3), 5 nM (P2X2/3) |
| Invitro | Ro-51 has highly selective for P2X 3 and P2X 2/3 exhibiting no antagonistic activity at other P2X receptor family members tested (P2X 1 , P2X 2 , P2X 4 , P2X 5 , and P2X 7 ) at concentrations up to 10 μM[1].RO51 also shows a significant drop in potency on human P2X3 receptors (IC50 = 110.5 and 0.04 nM, respectively for human and rat P2X3)[2]. |
| In Vivo | Ro-51 suffers rapid clearance, short half-lives, and high protein binding in rat[1]. Animal Model: |
| Name | Ro-51 |
| CAS | 1050670-85-3 |
| Formula | C17H23IN4O4 |
| Molar Mass | 474.29 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Alam Jahangir,et al. Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1632-5. [2]. Alexandre Serrano, et al. Differential Expression and Pharmacology of Native P2X Receptors in Rat and Primate Sensory Neurons. J Neurosci. 2012 Aug 22; 32(34): 11890–11896. |