| CAS NO: | 346692-04-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 307.4 |
| Cas No. | 346692-04-4 |
| Formula | C16H18FNO2S |
| Solubility | ≤100mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | N-(4-butylphenyl)-4-fluoro-benzenesulfonamide |
| Canonical SMILES | FC1=CC=C(S(NC2=CC=C(CCCC)C=C2)(=O)=O)C=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
DC260126 is a GPR40 antagonist [1][2].
The G protein-coupled receptor 40 (GPR40), also known as FFAR1, is a free fatty acid receptor, which is activated by saturated and unsaturated long or medium chain fatty acids in pancreatic β-cells. Free fatty acids (FFAs) are essential regulators of normal β-cell and play important roles in the pathogenesis of β-cell dysfunction in type 2 diabetes. GPR40 is a new potential drug target for the treatment of type 2 diabetes [1][2].
DC260126 is a FFAR1/GPR40 antagonist. DC260126 dose-dependently inhibited GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid with IC50 values of 6.28 ± 1.14, 5.96 ± 1.12, 7.07 ± 1.42 and 4.58 ± 1.14 μM, respectively. In GPR40-CHO cells, DC260126 dose-dependently reduced GTP-loading and ERK1/2 phosphorylation stimulated by linoleic acid. In Min6 cells, DC260126 inhibited palmitic acid potentiated glucose-stimulated insulin secretion, and negatively regulated GPR40 mRNA expression induced by oleic acid [1].
In obese diabetic db/db mice, DC260126 (10 mg/kg, 21-days treatment) significantly inhibited glucose stimulated insulin secretion, reduced blood insulin level and improved insulin sensitivity. DC260126 also reduced the apoptotic rate of pancreatic β-cells and the proinsulin/insulin ratio [2].
References:
[1]. Hu H, He LY, Gong Z, et al. A novel class of antagonists for the FFAs receptor GPR40. Biochem Biophys Res Commun. 2009 Dec 18;390(3):557-63.
[2]. Sun P, Wang T, Zhou Y, et al. DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic β-Cells dysfunction in db/db mice. PLoS One. 2013 Jun 11;8(6):e66744.
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