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AF-353 is a novel, potent and orally bioavailable P2X3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). AF-353 administered orally to rats and found to produce highly significant prevention and reversal of bone cancer pain behaviour. AF-353 is an excellent in vivo tool compound for study of these channels in animal models and demonstrates the feasibility of identifying and optimizing molecules into potential clinical candidates, and, ultimately, into a novel class of therapeutics for the treatment of pain-related disorders.
| Molecular Weight | 400.21 |
| Formula | C14H17IN4O2 |
| CAS Number | 865305-30-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related P2 Receptor Products |
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| NF449
NF449 is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. |
| NF279
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. |
| NF110
NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). |
| PSB-12062
PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4. |
| NF449 octasodium
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. |
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