AS 1269574
目录号 : GC12018
Agonist of GPR119
Cas No.:330981-72-1
Sample solution is provided at 25 µL, 10mM.
AS 1269574,(2-[2-(4-bromophenyl)-6-methylpyrimidin-4-yl] amino ethanol), was capable of inducing glucose-stimulated insulin secretion (GSIS) and improved glucose tolerance in normal mice. AS 1269574 is an agonist of GPR119 with EC50 value of 2.5 µM [1] [2].
GPR119 is highly expressed in pancreatic β-cells. This receptor enhances the effect of GSIS via the elevation of intracellular cAMP concentrations [2].
Treated with either 1 or 10 µM AS 1269574 for 20 min, the insulin secretion of mouse pancreatic MIN-6 β-cells pre-exposed to 16.8 mM glucose was significantly increased compared with the DMSO vehicle control. In contrast, AS 1269574 did not affect the insulin release of MIN-6 cells previously treated with low-glucose (2.8 mM) [2].
In normal mice, a single treatment with 100 mg/kg of AS 1269574 significantly reduced the area under the curve (AUC) after 2 h (AUC0-2h) of blood glucose. AS 1269574 significantly increase the plasma insulin AUC0-2h in mice compared with the vehicle control. A single oral administration of 100 mg/kg AS 1269574 did not significantly lower the blood glucose AUC in either fasted or fed mice, indicating AS 1269574 did not have a hypoglycemic effect [2].
References:
[1]. Shigeru Yoshida, Hirotsugu Tanaka, Hiroyuki Oshima, et al. AS1907417, a novel GPR119 agonist, as an insulinotropic and β-cell preservative agent for the treatment of type 2 diabetes. Biochemical and Biophysical Research Communications, 2010, 400: 745-751.
[2]. Shigeru Yoshida, Takahide Ohishi, Tetsuo Matsui, et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochemical and Biophysical Research Communications, 2010, 400: 437-441.
Cas No. | 330981-72-1 | SDF | |
化学名 | 2-((2-(4-bromophenyl)-6-methylpyrimidin-4-yl)amino)ethanol | ||
Canonical SMILES | BrC1=CC=C(C=C1)C2=NC(C)=CC(NCCO)=N2 | ||
分子式 | C13H14BrN3O | 分子量 | 308.17 |
溶解度 | DMF: 30 mg/ml,DMF:PBS (pH 7) (1:10): 0.1 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 3.245 mL | 16.2248 mL | 32.4496 mL |
5 mM | 0.649 mL | 3.245 mL | 6.4899 mL |
10 mM | 0.3245 mL | 1.6225 mL | 3.245 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.50%
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