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AS 1269574 Sale

目录号 : GC12018

Agonist of GPR119

AS 1269574 Chemical Structure

Cas No.:330981-72-1

规格 价格 库存 购买数量
1mg
¥261.00
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5mg
¥765.00
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10mg
¥1,326.00
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25mg
¥2,549.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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.

Chemical Properties

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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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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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
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