Grapiprant 是一种选择性EP4 受体拮抗剂，生理配体为前列腺素 E2(PGE2)，有用于骨关节炎疼痛和炎症的研究潜力。它取代 [3H]-PGE2(1 nM) 与狗的重组EP4 受体结合，IC50为 35 nM，Ki为 24 nM。

Grapiprant is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor (IC50: 35 nM, Ki: 24 nM).

Grapiprant (0-50 mg/kg; p.o; every 24 hours; for 9 months; beagles) is safe for dogs by long-term oral administration [2].

Animal Model: 36 beagles of both sexes (9-month-old). Dosage: 0 mg/kg, 1 mg/kg, 6 mg/kg, or 50 mg/kg. Administration: Oral administration; every 24 hours; for 9 months [2]

415903-37-6

C26H29N5O3S

491.61

RQ-00000007;CJ-023423;AAT-007

DMSO:48 mg/mL (97.64 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years