Grapiprant

Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2) . Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment[1][2][3] .

Product Specifications

CAS Number

[415903-37-6]

Product Name Alternative

CJ-023423; RQ-00000007; AAT-007

UNSPSC

12352005

Hazard Statement

H302

Target

Prostaglandin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Endocrinology; Cancer

Assay Protocol

https://www.medchemexpress.com/Grapiprant.html

Purity

99.57

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=S(C1=CC=C(C)C=C1)(NC(NCCC2=CC=C(N3C(CC)=NC4=C3C=C(C)N=C4C)C=C2)=O)=O

Molecular Formula

C26H29N5O3S

Molecular Weight

491.61

Precautions

H302

References & Citations

[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]Nagahisa A, et al. Pharmacology of grapiprant, a novel EP4 antagonist: receptor binding, efficacy in a rodent postoperative pain model, and a dose estimation for controlling pain in dogs. J Vet Pharmacol Ther. 2017 Jun;40 (3) :285-292.|[3]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.