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GPR120 Agonist 2

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Chemical Structure| 1234844-11-1 同义名 : -
CAS号 : 1234844-11-1
货号 : A748720
分子式 : C22H25ClO4
纯度 : 99%+
分子量 : 388.885
MDL号 : MFCD31619282
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 G protein-coupled receptor 120 (GPR120) is a Gαq coupled GPCR specifically activated by long-chain fatty acids (LCFAs). Upon stimulation by LCFAs, GPR120 can directly or indirectly modulate hormone secretion from the gastrointestinal tract and pancreas, and regulate lipid and/or glucose metabolism in adipose, liver, and muscle tissues. Additionally, GPR120 is postulated to mediate anti-inflammatory and insulin-sensitizing effects in adipose and macrophages[1]. GPR120 Agonist 2 is a GPR120 agonist which is useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. Agonism of GPR120 can reduce inflammation by inhibiting the expression of IL-6 and IL-8 induced by IL-1β[2]. GPR120 agonism correlates with prevention of the occurrence and development of metabolic disorders such as obesity and diabetes. GPR120 activation directly or indirectly inhibits inflammation, modulates hormone secretion from the gastrointestinal tract and pancreas, and regulates lipid and/or glucose metabolism in adipose, liver, and muscle tissues[3]. GPR120 agonist-treated wild-type, but not IL10-deficient and Blimp1-deficient, T helper type 1 cells induced less severe colitis. Furthermore, oral administration of GPR120 agonist protected mice from intestinal inflammation in both prevention and treatment schemes[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02444910 Diabetes Mellitus, Type 2 Phase 2 Completed - United States, Kentucky ... 展开 >> University of Kentucky's Center for Clinical and Translational Science (CCTS) Lexington, Kentucky, United States, 40536-0298 收起 <<
NCT03774095 Type 2 Diabetes Mellitus ... 展开 >> Obesity 收起 << Not Applicable Recruiting December 30, 2018 Denmark ... 展开 >> Odense University Hospital Recruiting Odense, Denmark, 5000 Contact: Karina Sørensen, MSc    26924602       Contact: Kurt Højlund, MD    +45 65413422 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.71mL

5.14mL

2.57mL
参考文献

[1] Xuqing Zhang, Mark J Macielag. GPR120 agonists for the treatment of diabetes: a patent review (2014 present).Expert Opin Ther Pat. 2020 Oct;30(10):729-742.

[2] Zhixian Xu,et al. Agonism of GPR120 prevented IL-1β-induced reduction of extracellular matrix through SOX-9. Aging (Albany NY). 2020 Jun 24;12(12):12074-12085.

[3]Dan Zhang, Po Sing Leung. Potential roles of GPR120 and its agonists in the management of diabetes.

[4]Wenjing Yang,et al. GPR120 Inhibits Colitis Through Regulation of CD4 + T Cell Interleukin 10 Production. Gastroenterology. 2021 Sep 16;S0016-5085(21)03497-1.