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Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. Grapiprant has Ki values of 13 nM and 20 nM against human EP4 and rat EP4, respectively.
In vitro, Grapiprant inhibits [(3)H]PGE(2) binding to both human and rat EP(4) receptors with K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively. Grapiprant is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. Grapiprant also inhibits PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 +/- 0.03 and 8.2 +/- 0.2 nM, respectively.
In vivo, oral administration of Grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).
| Molecular Weight | 491.61 |
| Formula | C26H29N5O3S |
| CAS Number | 415903-37-6 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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