Grapiprant, EP4 receptor antagonist (TBI4006)

Description

Product Details

Formal 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

Molecular Formula: C₂₆H₂₉N₅O₃S

Formula Weight: 491.61

CAS Number: 415903-37-6

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 10 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

EP4 receptor antagonist.

Functions

Grapiprant (415903-37-6) is a potent (Ki = 13 nM for human and 20 nM for rat) and selective prostaglandin EP4 receptor antagonist. It produces antihyperalgesic effects in animal models of pain, and has significant anti-inflammatory effects in a rat model of adjuvant-induced arthritis. 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. Grapiprant/Pembrolizumab combination is in clinical trials for advanced or metastatic NSCLC adenocarcinoma.

Application Procedures

First dissolved in DMSO (up to at least 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.