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Grapiprant

Overview
Catalog # bs-82750c-5-mg
Product Name Grapiprant
Specifications
Storage Buffer Off-white solid
Storage Condition -20°C
Target
Product Information 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
Description CAS Number: 415903-37-6

Chemical Name: 1—[2-[4-(2-Ethyl-4,6-dimethylimidazo[4,5-c]pyridine-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea

Molecular weight: 491.61

Formula: C26H29N5O3S

Solubility: DMSO (>10 mg/ml)

Physical Properties: Off-white solid

Purity: 98% by TLC NMR (Conforms)