CJ-42794是前列腺素受体EP4的选择性拮抗剂, 抑制[3H]-PGE2与EP4受体结合的平均pKi为8.5, 对EP4选择性比EP1, EP2和EP3高200多倍。

CJ-42794 is a selective antagonist of prostaglandin E receptor subtype 4 (EP4). It inhibits [3H]-PGE2 binding to the human EP4 receptor (a mean pKi: 8.5). CJ-42794 is a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3) (IC50 : 8.5 (pKi )).

CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor (mean pA2: 8.6). CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner [1].

CJ-42794 significantly delays ulcer healing in rats and mice and these responses were both attenuated by coadministration of CJ-42794 [2].

847728-01-2

C22H17ClFNO4

413.83

CJ-042794

DMSO:28 mg/mL (67.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years