GSK 137647
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.
靶点:FFA4/GPR120
IC50: N/A
GSK137647A是FFA4/GPR120的有效选择性激动剂,对人、小鼠和大鼠受体的pEC50分别为6.3、6.2和6.1[1]。游离脂肪酸受体4(FFA4/GPR120)属于G蛋白偶联受体家族的成员,是潜在的7TM受体,参与长链脂肪酸刺激的胰高血糖素样肽-1(GLP-1)的分泌。FFA4在肠内分泌细胞系STC-1和肠中高表达[1]。GLP-1调节多种生理功能,包括饮食行为[2]。
体外实验:在MIN6小鼠胰岛细胞中,GSK137647A(50 μM)以浓度依赖性方式诱导葡萄糖(25 mM)刺激的胰岛素分泌增加[1]。此外,在人体肠道细胞系NCI-H716中,100 μM的GSK137647A诱导GLP-1分泌的适度增加。此外,在U2OS细胞中,GSK137647A诱导细胞内钙离子的积累[1]。
体内实验:GSK137647A(50 μM)诱导小鼠轮廓乳头(CVPs)中活性GLP-1的释放[2]。
参考文献:
1. Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3.
2. Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res. 2012;53(11):2256-65.
Physical Appearance | A crystalline solid |
Storage | Store at RT |
M.Wt | 305.39 |
Cas No. | 349085-82-1 |
Formula | C16H19NO3S |
Solubility | insoluble in H2O; ≥121.6 mg/mL in DMSO; ≥9.49 mg/mL in EtOH with ultrasonic |
Chemical Name | N-mesityl-4-methoxybenzenesulfonamide |
SDF | Download SDF |
Canonical SMILES | CC1=CC(C)=C(NS(C2=CC=C(OC)C=C2)(=O)=O)C(C)=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。 |
质量控制和MSDS
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