Chemical Name: 1-[2-[4-(2-Ethyl-4,6-dimethylimidazo[4,5-c]pyridine-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea. Alternate Names: CJ-023,423, ARY-007
EP4 receptor antagonist.
Molecular Weight:
491.61
Purity:
98% by TLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[415903-37-6]
Formula:
C26H29N5O3S
Application Notes:
Grapiprant is a potent (Ki = 13 nM for human and 20 nM for rat) and selective prostaglandin EP4 receptor antagonist.1 It produces antihyperalgesic effects in animal models of pain, and has significant anti-inflammatory effects in a rat model of adjuvant-induced arthritis.2 EP4 receptors have been shown to be involved in PGE2 stimulation of Th1 differentiation and Th17 expansion revealing a potential role for PGE2 receptors in immunosuppression.3,4 Grapiprant/Pembrolizumab combination is in clinical trials for advanced or metastatic NSCLC adenocarcinoma.5
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