415903-37-6

• 常用中文名：Grapiprant
• 常用英文名：grapiprant
• CAS号：415903-37-6
• 分子式：C₂₆H₂₉N₅O₃S
• 分子量：491.605
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 前列腺素受体
• 发布时间：2017-11-30 15:10:11
• 更新时间：2024-01-04 17:42:36
• Grapiprant是一种选择性EP4受体拮抗剂, 生理配体为前列腺素E2(PGE2)。

名称

• 中文名: Grapiprant
• 英文名: Grapiprant
• 英文别名: N-{2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}-N'-[(4-methylphenyl)sulfonyl]urea; CJ-023,423; MR10A7; N-({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}carbamoyl)-4-methylbenzenesulfonamide; grapiprant; Benzenesulfonamide, N-[[[2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]amino]carbonyl]-4-methyl-; RQ-00000007; AAT-007; UNII:J9F5ZPH7NB; 2-Ethyl-4,6-dimethyl-1-[4-[2-[[[[(4-methylphenyl)sulfonyl]amino]carbonyl]amino]ethyl]phenyl]-1H-imidazo[4,5-c]pyridine

物化性质

• 密度: 1.3±0.1 g/cm3
• 分子式: C₂₆H₂₉N₅O₃S
• 分子量: 491.605
• 精确质量: 491.199097
• LogP: 4.56
• 折射率: 1.647
• 储存条件: 2-8℃

生物活性

• 描述: Grapiprant是一种选择性EP4受体拮抗剂, 生理配体为前列腺素E2(PGE2)。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体
  研究领域 >> 代谢疾病
• 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]. 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]. Rahman MJ, et al. Restoration of the type I IFN-IL-1 balance through targeted blockade of PTGER4 inhibits autoimmunity in NOD mice. JCI Insight. 2018 Feb 8;3(3). pii: 97843.