Grapiprant
| CAS No. | 415903-37-6 | Cat. No. | BCP20570 |
| Name | Grapiprant | ||
| Synonyms | CJ-023423; CJ 023423; CJ023423;RQ-00000007; RQ 00000007; RQ00000007; AAT-007; AAT007; AAT 007; | ||
| Formula | C26H29N5O3S | M. Wt | 491.61 |
| Description | Grapiprant, also known as CJ-023,423, RQ-00000007 and AAT-007, is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. In vitro, CJ-023,423 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. CJ-023,423 is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. It 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 CJ-023,423 significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg). | ||
| Pathways | GPCR/G Protein | ||
| Targets | Prostaglandin Receptor | ||
Structure
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