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产品描述： 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 |
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靶点：
dog EP4:35 nM (IC50);dog EP4:24 nM (Ki);ProstaglandinReceptor |
体内研究：
Grapiprant (0-50 mg/kg; oral administration; every 24 hours; for 9 months; beagles) is safe for dogs by long-term oral administration. Efficacy of Grapiprant in the treatment of dogs with osteoarthritis needs to be evaluated in other studies. 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 Result: Long-term oral administration was safe for dogs. |
参考文献：
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. |
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溶解性：
soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.034 ml |
10.171 ml |
20.342 ml |
| 5 mM |
0.407 ml |
2.034 ml |
4.068 ml |
| 10 mM |
0.203 ml |
1.017 ml |
2.034 ml |
| 50 mM |
0.041 ml |
0.203 ml |
0.407 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京