GW9508
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.
GW9508是一种选择性的GPR40和120激动剂,pEC50值分别为7.32 ± 0.03和5.46 ± 0.09[1]。
GPR40/120属于G蛋白偶联受体(GPCRs)家族,可被游离脂肪酸激活。粘膜炎症引发GPR40、GPR120和一些炎性细胞因子的过表达,并与回肠肿瘤坏死因子(TNF)-α和GPR表达水平相关[2][3]。
GW9508是GPR40/120的激动剂,与已报道的GPR40/120激动剂GW1100不同。使用表达GPR40或GRP120的HEK-293(人胚肾)细胞试验时,GW9508通过剂量依赖的方式活化GPR40/120,提高胞内Ca2+浓度[1]。在大鼠胰脏β细胞中,GW9508疗法通过激活GPR40和GPR120,激活KATP通道,抑制GSIS[4]。在TNF-α处理的大鼠L细胞中,施用GW9508通过活化GPR40和120,提高GLP-2的表达量[2]。
参考文献:
[1]. Briscoe, C.P., et al., Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol, 2006. 148(5): p. 619-28.
[2]. Tsukahara, T., et al., Tumor necrosis factor alpha decreases glucagon-like peptide-2 expression by up-regulating G-protein-coupled receptor 120 in Crohn disease. Am J Pathol, 2015. 185(1): p. 185-96.
[3]. Habib, A.M., et al., Co-localisation and secretion of glucagon-like peptide 1 and peptide YY from primary cultured human L cells. Diabetologia, 2013. 56(6): p. 1413-6.
[4]. Zhao, Y.F., et al., GW9508 inhibits insulin secretion by activating ATP-sensitive potassium channels in rat pancreatic beta-cells. J Mol Endocrinol, 2013. 51(1): p. 69-77.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 347.41 |
Cas No. | 885101-89-3 |
Formula | C22H21NO3 |
Solubility | insoluble in H2O; ≥16.05 mg/mL in DMSO; ≥49.1 mg/mL in EtOH |
Chemical Name | 3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C=C1)OC2=CC=CC(=C2)CNC3=CC=C(C=C3)CCC(=O)O |
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。 |
Description | GW9508是一种小分子的GPR40和GPR120激动剂,EC50值分别为47 nM和2.2 ?M。 | |||||
靶点 | GPR40 | GPR120 | ||||
IC50 | 47 nM (EC50) | 2.2 ?M (EC50) |
质量控制和MSDS
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