GSK1292263
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.
GSK1292263是一种新型GPR119受体激动剂,用于II型糖尿病的治疗。
GPR119是A类(视紫红质型)孤儿GPCR,与人类基因组无密切的序列相关性。GPR119的活化提高胞内cAMP的积累,导致胰腺β细胞胰岛素的分泌增加以及肠肽GLP-1(胰高血糖素样肽1)、GIP(葡萄糖依赖性促胰岛素肽)和PYY(多肽YY)的释放增加。
体外实验:GSK1292263处理几乎不抑制CYPs (CYP1A2、2C9、2C19、2D6、3A4)、p-GP、OATP1B3和OCT2。但是GSK1292263能够抑制BCRP和OATP1B1,二者是参与他汀类药物转运的转运蛋白[1]。
体内试验:在大鼠中进行葡萄糖耐受实验,相比于对照组,给予GSK1292263显著增强峰值胰岛素应答和胰岛素AUC (0-15 min)。胰岛素的上调与葡萄糖代谢清除率相关。通过高胰岛素-正葡萄糖钳夹术,胰岛素灌注前2小时按10或30 mg/kg的剂量给予Sprague-Dawley大鼠GSK1292263能促进胰高血糖素分泌,同时不提高血糖水平[2]。
参考文献:
1. Polli JW, Hussey E, Bush M, et al. Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: from in vitro data to clinical study design. Xenobiotica; the fate of foreign compounds in biological systems. 2013;43(6):498-508.
2. Zhu X, Huang D, Lan X, et al. The first pharmacophore model for potent G protein-coupled receptor 119 agonist. European journal of medicinal chemistry. 2011;46(7):2901-2907.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 456.56 |
Cas No. | 1032823-75-8 |
Formula | C23H28N4O4S |
Solubility | ≥21.1 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 5-[4-[[6-(4-methylsulfonylphenyl)pyridin-3-yl]oxymethyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole |
SDF | Download SDF |
Canonical SMILES | CC(C)C1=NOC(=N1)N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(=O)(=O)C |
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 | GSK1292263是一种新型GPR119激动剂。 | |||||
靶点 | GPR119 | |||||
IC50 |