415903-37-6

415903-37-6 structure

Name: grapiprant
Chemical Name: Grapiprant
CAS Number: 415903-37-6
Molecular Formula: C₂₆H₂₉N₅O₃S
Molecular Weight: 491.605
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2017-11-30 15:10:11
Modify Date: 2024-01-04 17:42:36
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]

Name	Grapiprant
Synonyms	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

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.