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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.
| Cell Experiment | |
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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 |
|---|
| Prasugrel hydrochloride
Prasugrel hydrochloride is a novel inhibitor of platelet activation and aggregation. |
| GW 791343 dihydrochloride
GW 791343 dihydrochloride is a non-competitive inhibitor of human P2X(7) receptor. |
| Prasugrel
Prasugrel is a platelet inhibitor irreversibly binding to P2Y12 receptors. |
| MRS 2578
MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
| PPADS Tetrasodium
PPADS tetrasodium salt is a non-selective P2 purinergic antagonist blocking recombinant P2X1, P2X2, P2X3, P2X5 with IC50 of 1-2.6 μM, native P2Y2-like with IC50 of ~ 0.9 mM, and recombinant P2Y4 receptors with IC50 of ~ 15 mM |
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