RO-3
CAS No. : 1026582-88-6
| Size | Price | Stock |
|---|---|---|
| 5mg | $80 | In-stock |
| 10mg | $150 | In-stock |
| 25mg | $350 | In-stock |
| 50mg | $630 | In-stock |
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| 200 mg | Get quote | |
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| Cat. No. : | HY-19978 |
| M.Wt: | 302.37 |
| Formula: | C16H22N4O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 125 mg/mL (ultrasonic;warming;heat to 60°C) |
RO-3 is a potent, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7)[1].
IC50 & Target:pIC50: 5.9 (human homomultimeric P2X3 receptor); 7.0 (human heteromultimeric P2X2/3 receptor)[1]
In Vivo:In a guinea pig ureter-afferent nerve preparation, and mouse bladder-pelvic nerve preparation, RO-3 dose-dependently reduces afferent nerve activity induced by distension or α,β-meATP[1].
RO-3 has activity in several rodent models of pain, as well as in cystometry models optimized to measure various parameters associated with sensory regulation of the micturition reflex[1].
RO-3 has moderate to high metabolic stability in rat and human hepatocytes and liver microsomes, and is highly permeable, orally bioavailable (14%), and has a reasonable in vivo plasma half-life (t1/2=0.41 h) in rats[1].
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