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AS 1269574
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AS 1269574图片
CAS NO:330981-72-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
AS 1269574 是一种有效的口服 GPR119 激动剂,在表达人 GPR119 的 HEK293 细胞中的 EC50 为 2.5 μM。
Cas No.330981-72-1
化学名2-((2-(4-bromophenyl)-6-methylpyrimidin-4-yl)amino)ethanol
Canonical SMILESBrC1=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
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.