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grapiprant

Names

[ CAS No. ]:
415903-37-6

[ Name ]:
grapiprant

[Synonym ]:
N-{2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}-N'-[(4-methylphenyl)sulfonyl]urea
CJ-023,423
MR10A7
N-({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}carbamoyl)-4-methylbenzenesulfonamide
grapiprant
Benzenesulfonamide, N-[[[2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]amino]carbonyl]-4-methyl-
RQ-00000007
AAT-007
UNII:J9F5ZPH7NB
2-Ethyl-4,6-dimethyl-1-[4-[2-[[[[(4-methylphenyl)sulfonyl]amino]carbonyl]amino]ethyl]phenyl]-1H-imidazo[4,5-c]pyridine

Biological Activity

[Description]:

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2).Target: prostaglandin receptorin vitro: Grapiprant is a novel pharmacologically active ingredient, acts as a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). [1]in vivo: Grapiprant is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis. [1] Results suggested the safety of long-term oral administration of grapiprant to dogs. Efficacy of grapiprant in the treatment of dogs with osteoarthritis needs to be evaluated in other studies. [2]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor
Research Areas >> Metabolic Disease

[References]

[1]. Vito VD, et al. Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection. J Pharm Biomed Anal. 2016 Jan 25;118:251-8.

[2]. Rausch-Derra LC, et al. Evaluation of the safety of long-term, daily oral administration of grapiprant, a novel drug for treatment of osteoarthritic pain and inflammation, in healthy dogs. Am J Vet Res. 2015 Oct;76(10):853-9.

[3]. Rahman MJ, et al. Restoration of the type I IFN-IL-1 balance through targeted blockade of PTGER4 inhibits autoimmunity in NOD mice. JCI Insight. 2018 Feb 8;3(3). pii: 97843.


[Related Small Molecules]

Dinoprostone | Prostaglandin E1 | E7046 | ONO-AE3-208 | PF 04418948 | Fevipiprant | TG6-10-1 | Taprenepag | GW 627368 | MRE-269 | Ramatroban | AH 6809 | Laropiprant | AZD1981 | Evatanepag

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C26H29N5O3S

[ Molecular Weight ]:
491.605

[ Exact Mass ]:
491.199097

[ LogP ]:
4.56

[ Index of Refraction ]:
1.647

[ Storage condition ]:
2-8℃

Related Compounds