Grapiprant Inhibitor

Grapiprant (CJ-023423) is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1nM) binding to dog recombinant EP4 receptor (IC50: 35nM, Ki: 24nM).

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.
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.
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.
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.
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.
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.

Small volumes of Grapiprant, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5764540 is an inhibitor targeting Grapiprant.