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AS 2034178
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 2034178图片
CAS NO:1030846-42-4
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
AS 2034178 是一种特异性的口服活性 GPR40 激动剂,具有葡萄糖依赖性胰岛素分泌增强作用。
Cas No.1030846-42-4
化学名3-(2-fluoro-4-(((1-(2-phenoxyethyl)-1,2,3,4-tetrahydroquinolin-5-yl)methyl)amino)phenyl)propanoic acid
Canonical SMILESFC1=C(CCC(O)=O)C=CC(NCC(C=CC=C23)=C2CCCN3CCOC4=CC=CC=C4)=C1
分子式C27H29FN2O3
分子量448.53
溶解度<22.43mg/ml in DMSO;<8.97mg/ml in ethanol
储存条件Store at -20℃
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

AS2034178 is a GPR40 agonist [1] with an hEC50 value of 380 nM [2].

GPR40 is a receptor of free fatty acid. It regulates glucose-dependent insulin secretion [1].

AS2034178 can improve glucose homeostasis and maintain or enhance islet beta cell functions [3]. AS2034178 demonstrated highly and dose-dependently increase in intracellular Ca2+ levels [1]. The maximum efficacy of the increase in Ca2+ was nearly equal to that of an endogenous ligand of GPR40, namely linolenic acid. But the potency of AS2034178 was much higher than that of linolenic acid. Human GPR41-, GPR43-, GPR119-, and GPR120-overexpressing CHO cells were developed to evaluate the increase of intracellular Ca2+ concentration caused by AS2034178. Only GPR40-expressing cells showed increased intracellular Ca2+. In pancreas b-cell–derived MIN6 cells, AS2034178 dose-dependently and significantly induced insulin secretion only under high-glucose conditions (22.4 mM) [1].

In ob/ob mice, chronic treatment with AS2034178 significantly improved whole-body glucose metabolism, insulin, HbA1c, and pancreatic insulin levels [2]. In normal mice, AS2034178 at 0.3 to 10 mg/kg dose-dependently induced the suppression of plasma-glucose increases after oral administration with glucose, and the area decrease under the plasma glucose concentration-time curve was significant at doses over 1 mg/kg. After oral glucose administration, plasma insulin levels increased and at 5 minutes after glucose administration were dose-dependently and significantly increased at AS2034178 dosages over 3 mg/kg [1].

References:
[1].  Tanaka H, Yoshida S, Oshima H, et al. Chronic treatment with novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion[J]. Journal of Pharmacology and Experimental Therapeutics, 2013, 346(3): 443-452.
[2].  Defossa E, Wagner M. Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus[J]. Bioorganic & medicinal chemistry letters, 2014, 24(14): 2991-3000.
[3].  Milligan G, Alvarez-Curto E, Watterson KR, et al. Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4[J]. British journal of pharmacology, 2015, 172(13): 3254-3265.