Grapiprant

• CAT Number: I003508
• CAS Number: 415903-37-6
• Molecular Formula: C26H29N5O3S
• Molecular Weight: 491.6
• Purity: ≥95%
• Synonyms: N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide
• Target: Prostaglandin Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• InChI: InChI=1S/C26H29N5O3S/c1-5-24-29-25-19(4)28-18(3)16-23(25)31(24)21-10-8-20(9-11-21)14-15-27-26(32)30-35(33,34)22-12-6-17(2)7-13-22/h6-13,16H,5,14-15H2,1-4H3,(H2,27,30,32)
• InChIKey: HZVLFTCYCLXTGV-UHFFFAOYSA-N
• SMILES: O=C(NS(C1=CC=C(C)C=C1)(=O)=O)NCCC2=CC=C(N3C(CC)=NC4=C(C)N=C(C)C=C43)C=C2

Grapiprant (CAT: I003508) is a pharmaceutical compound belonging to the class of nonsteroidal anti-inflammatory drugs (NSAIDs). It acts as a selective antagonist of the prostaglandin EP4 receptor, which plays a role in mediating pain and inflammation. Grapiprant is primarily used in veterinary medicine for the treatment of pain and inflammation associated with osteoarthritis in dogs. By selectively blocking the EP4 receptor, Grapiprant helps to reduce pain and inflammation without affecting other prostaglandin pathways. It provides a targeted approach to managing osteoarthritis symptoms in dogs, improving their mobility and overall quality of life.

Reference

1:Pharmacokinetics of grapiprant, a selective EP4 prostaglandin PGE2 receptor antagonist, after 2 mg/kg oral and i.v. administrations in cats. Lebkowska-Wieruszewska B, De Vito V, Owen H, Poapholatep A, Giorgi M.J Vet Pharmacol Ther. 2017 Apr 29. doi: 10.1111/jvp.12414. [Epub ahead of print] PMID: 28459136 2:Pharmacokinetic/pharmacodynamic evaluation of grapiprant in a carrageenan-induced inflammatory pain model in the rabbit. De Vito V, Salvadori M, Poapolathep A, Owen H, Rychshanova R, Giorgi M.J Vet Pharmacol Ther. 2016 Dec 7. doi: 10.1111/jvp.12380. [Epub ahead of print] PMID: 27925221 3:Pharmacokinetic comparison of oral tablet and suspension formulations of grapiprant, a novel therapeutic for the pain and inflammation of osteoarthritis in dogs. Rausch-Derra LC, Rhodes L, Freshwater L, Hawks R.J Vet Pharmacol Ther. 2016 Dec;39(6):566-571. doi: 10.1111/jvp.12306. Epub 2016 Mar 29. PMID: 27027634 4:Pharmacokinetics and estimated bioavailability of grapiprant, a novel selective prostaglandin E2 receptor antagonist, after oral administration in fasted and fed dogs. Łebkowska-Wieruszewska B, Barsotti G, Lisowski A, Gazzano A, Owen H, Giorgi M.N Z Vet J. 2017 Jan;65(1):19-23. Epub 2016 Oct 19. PMID: 27691904 5: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. Nagahisa A, Okumura T.J Vet Pharmacol Ther. 2017 Jun;40(3):285-292. doi: 10.1111/jvp.12349. Epub 2016 Sep 6. PMID: 27597397 6:Safety and toxicokinetic profiles associated with daily oral administration of grapiprant, a selective antagonist of the prostaglandin E2 EP4 receptor, to cats. Rausch-Derra LC, Rhodes L.Am J Vet Res. 2016 Jul;77(7):688-92. doi: 10.2460/ajvr.77.7.688. PMID: 27347820 7:A Prospective, Randomized, Masked, Placebo-Controlled Multisite Clinical Study of Grapiprant, an EP4 Prostaglandin Receptor Antagonist (PRA), in Dogs with Osteoarthritis. Rausch-Derra L, Huebner M, Wofford J, Rhodes L.J Vet Intern Med. 2016 May;30(3):756-63. doi: 10.1111/jvim.13948. Epub 2016 Apr 13. PMID: 27075237 Free PMC Article8:Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection. De Vito V, Saba A, Lee HK, Owen H, Poapolathep A, Giorgi M.J Pharm Biomed Anal. 2016 Jan 25;118:251-8. doi: 10.1016/j.jpba.2015.11.004. Epub 2015 Nov 7. PMID: 26580822 9: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. Rausch-Derra LC, Huebner M, Rhodes L.Am J Vet Res. 2015 Oct;76(10):853-9. doi: 10.2460/ajvr.76.10.853. PMID: 26413822