AS 2034178
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AS2034178是GPR40的激动剂[1],hEC50值为380 nM [2]。
GPR40是游离脂肪酸的受体。它调节葡萄糖依赖性的胰岛素分泌[1]。
AS2034178可以改善葡萄糖稳态,维持或增强胰岛β细胞功能[3]。 AS2034178可以高效且以剂量依赖性的方式增加细胞内Ca2+水平[1]。其对钙离子增加的最大功效几乎等于GPR40的内源性配体即亚麻酸的功效。但AS2034178的效力比亚麻酸高得多。在人类GPR41-、GPR43-、GPR119-和GPR120过表达的CHO细胞中,对AS2034178引起的细胞内钙离子浓度的增加进行评价。只有表达GPR40的细胞内Ca2+增加。在胰腺β细胞衍生的MIN6细胞中,仅在高葡萄糖条件下(22.4 mM),AS2034178以剂量依赖性方式显著诱导胰岛素分泌[1]。
在ob/ob小鼠中,用AS2034178慢性治疗显著改善全身葡萄糖代谢、胰岛素、HbA1c和胰腺胰岛素水平[2]。在正常小鼠中,葡萄糖口服给药后,0.3到10 mg/kg 的AS2034178以剂量依赖性方式抑制血浆葡萄糖的增加,超过1 mg/kg的剂量使血浆葡萄糖浓度-时间曲线下的面积显著减少。口服葡萄糖后,血浆胰岛素水平升高,在口服葡萄糖后5分钟时,超过3 mg/kg剂量的AS2034178以剂量依赖性方式显著增加血浆胰岛素水平 [1]。
参考文献:
[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.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 448.53 |
Cas No. | 1030846-42-4 |
Formula | C27H29FN2O3 |
Solubility | <22.43mg/ml in DMSO; <8.97mg/ml in ethanol |
Chemical Name | 3-(2-fluoro-4-(((1-(2-phenoxyethyl)-1,2,3,4-tetrahydroquinolin-5-yl)methyl)amino)phenyl)propanoic acid |
SDF | Download SDF |
Canonical SMILES | FC1=C(CCC(O)=O)C=CC(NCC(C=CC=C23)=C2CCCN3CCOC4=CC=CC=C4)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |