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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; | ||
SMILES | O=S(C1=CC=C(C)C=C1)(NC(NCCC2=CC=C(N3C(CC)=NC4=C3C=C(C)N=C4C)C=C2)=O)=O | ||
Chemical Name | |||
Formula | C26H29N5O3S | M. Wt | 491.61 |
Purity | 98% | Storage | Store at 4-8°C |
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). |
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