| Description | Grapiprant (AAT-007) is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor (IC50: 35 nM, Ki: 24 nM). |
| In vivo | Grapiprant（0-50 mg/kg；口服；每24小时一次；为期9个月；beagles）经长期口服给药对狗是安全的[2]。 |
| Animal experiments | Animal Model: 36 beagles of both sexes (9-month-old). Dosage: 0 mg/kg, 1 mg/kg, 6 mg/kg, or 50 mg/kg. Administration: Oral administration; every 24 hours; for 9 months [2] |
| Target activity | EP4:35 nM |
| Synonyms | AAT-007, RQ-00000007, CJ-023423 |
| molecular weight | 491.61 |
| Molecular formula | C26H29N5O3S |
| CAS | 415903-37-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 48 mg/mL (97.64 mM) |
| 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. 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. |