Grapiprant | EP4 Receptor antagonist
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $80.00 | ||
| 25 mg | $250.00 |
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
References/Citations:
1) Nakao et al. (2007), CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties; J. Pharmacol. Exp. Ther. 332 686
2) Okumura et al. (2008), Effects of the selective EP4 antagonist, CJ-023,423 on chronic inflammation and bone destruction in rat adjuvant-induced arthritis; J. Pharm. Pharmacol. 60 7235
3) Chen et al. (2010), A novel antagonist of the prostaglandin E2 EP4 receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models; Br. J. Pharmacol. 160 292
4) Wang and DuBois (2016), Wang and DuBois (2016), The Role of Prostaglandin E2 in Tumor-Associated Immunosuppression; Trends Mol. Med. 22 1
5) NCT03696212 and NCT03658772
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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
References/Citations:
1) Nakao et al. (2007), CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties; J. Pharmacol. Exp. Ther. 332 686
2) Okumura et al. (2008), Effects of the selective EP4 antagonist, CJ-023,423 on chronic inflammation and bone destruction in rat adjuvant-induced arthritis; J. Pharm. Pharmacol. 60 7235
3) Chen et al. (2010), A novel antagonist of the prostaglandin E2 EP4 receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models; Br. J. Pharmacol. 160 292
4) Wang and DuBois (2016), Wang and DuBois (2016), The Role of Prostaglandin E2 in Tumor-Associated Immunosuppression; Trends Mol. Med. 22 1
5) NCT03696212 and NCT03658772
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