Grapiprant

• UNSPSC Description:

  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] .

• Target Antigen:

  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

• 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 Weight:

  491.61

• 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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 2

• CAS Number:

  415903-37-6