AS 2034178
目录号 : GC11467
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
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 1030846-42-4 | SDF | |
| 化学名 | 3-(2-fluoro-4-(((1-(2-phenoxyethyl)-1,2,3,4-tetrahydroquinolin-5-yl)methyl)amino)phenyl)propanoic acid | ||
| Canonical SMILES | FC1=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2295 mL | 11.1475 mL | 22.2951 mL |
| 5 mM | 0.4459 mL | 2.2295 mL | 4.459 mL |
| 10 mM | 0.223 mL | 1.1148 mL | 2.2295 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。