Grapiprant | EP4 Receptor antagonist

CAS:
415903-37-6
Catalog Number:
10-4006
Activity:
EP4 Receptor antagonist
Chemical Name:
1—[2-[4-(2-Ethyl-4,6-dimethylimidazo[4,5-c]pyridine-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea
Alternate Names:
CJ-023423; ARY-007
Molecular Weight:
491.61
Molecular Formula:
C26H29N5O3S
Solubility:
Soluble in DMSO (up to at least 10 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
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

CAS:
415903-37-6
Catalog Number:
10-4006
Activity:
EP4 Receptor antagonist
Chemical Name:
1—[2-[4-(2-Ethyl-4,6-dimethylimidazo[4,5-c]pyridine-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea
Alternate Names:
CJ-023423; ARY-007
Molecular Weight:
491.61
Molecular Formula:
C26H29N5O3S
Solubility:
Soluble in DMSO (up to at least 10 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

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

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