纯度:98% by TLC;NMR (Conforms)
分子式:C26H29N5O3S
分子量:491.61
溶剂:DMSO (>10 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):EP4 receptor antagonist.
Function / Pharmacology:Grapiprant (415903-37-6) 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