733750-99-7

• 常用中文名：(2-氟-4-甲烷磺酰基-苯基)-{6-[4-(3-异丙基-[1,2,4]噁二唑-5-基)-哌啶-1-基]-5-硝基嘧啶-4-基}-胺
• 常用英文名：AR 231453
• CAS号：733750-99-7
• 分子式：C₂₁H₂₄FN₇O₅S
• 分子量：505.52300
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 GPR119
• 发布时间：2019-01-01 11:06:36
• 更新时间：2026-10-01 07:54:54
• AR231453是GPR119激动剂,能增强葡萄糖依赖的胰岛素分泌和GLP-1释放。

名称

• 中文名: (2-氟-4-甲烷磺酰基-苯基)-{6-[4-(3-异丙基-[1,2,4]噁二唑-5-基)-哌啶-1-基]-5-硝基嘧啶-4-基}-胺
• 英文名: N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine
• 中文别名: 231453,GPR119激动剂
• 英文别名: 4-Pyrimidinamine, N-[2-fluoro-4-(methylsulfonyl)phenyl]-6-[4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]-5-nitro; 231453; -231453; N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5; 231453, GPR119 agonist; inhibit,GPR119,-231453,G Protein-Coupled Rector 119,diabetes,231453, 231453,insulin,Inhibitor,HIT-,glucose,GPCR; N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-nitropyrimidin-4-amine; (2-FLUORO-4-METHANESULFONYL-PHENYL)-(6-[4-(3-ISOPROPYL-[1,2,4]OXADIAZOL-5-YL)-PIPERIDIN-1-YL]-5-NITRO-PYRIMIDIN-4-YL)-AMINE; N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-ni; 231453, 10 mM in DMSO; unii-07z1p4981i

物化性质

• 分子式: C₂₁H₂₄FN₇O₅S
• 分子量: 505.52300
• 精确质量: 505.15400
• PSA: 168.31000
• LogP: 5.30340
• 储存条件: 2-8℃

生物活性

• 描述: AR231453是GPR119激动剂,能增强葡萄糖依赖的胰岛素分泌和GLP-1释放。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GPR119
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. Chu ZL, et al. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology. 2007 Jun;148(6):2601-9.

  [2]. Chu ZL, et al. A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glucose-dependent insulinotropic Peptide release. Endocrinology. 2008 May;149(5):2038-47.

  [3]. Semple G, et al. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem. 2008 Sep 11;51(17):5172-5.

合成路线

832755-13-2 1054579-82-6 ~39% 733750-99-7

文献：Semple, Graeme; Fioravanti, Beatriz; Pereira, Guillherme; Calderon, Imelda; Uy, Jane; Choi, Karoline; Xiong, Yifeng; Ren, Albert; Morgan, Michael; Dave, Vibha; Thomsen, William; Unett, David J.; Xing, Charles; Bossie, Stuart; Carroll, Chris; Chu, Zhi-Liang; Grottick, Andrew J.; Hauser, Erin K.; Leonard, James; Jones, Robert M. Journal of Medicinal Chemistry, 2008 , vol. 51, # 17 p. 5172 - 5175

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