Grapiprant

• Background :

  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

• Conjugation :

  Unconjugated

• Buffer :

  Off-white solid

• Storage Conditions :

  -20°C