DC260126
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.
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.
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 |
SDF | Download SDF |
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。 |
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