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Gefapixant (AF-219) is an orally active small molecule antagonist at human P2X3-containing receptors, with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
In vivo, in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate), Gefapixant (7d bid, orally; right) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses.
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Rats |
| Formulation | |
| Dosages | 6, 20, and 60 mg/kg two times a day and continues up to a week |
| Administration | by intraplantar or oral |
| Molecular Weight | 353.40 |
| Formula | C14H19N5O4S |
| CAS Number | 1015787-98-0 |
| Solubility (25°C) | DMSO ≥ 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related P2 Receptor Products |
|---|
| 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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