Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK256073 是一种口服有活性的GPR109A 选择性激动剂,也是一种持久的人HCA2激动剂(pEC50:7.5) 。它能够减少脂降解,而显著改善葡萄糖稳态,对 2 型糖尿病和血脂异常具有潜在的研究价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 597 | 现货 | ||
2 mg | ¥ 878 | 现货 | ||
5 mg | ¥ 1,490 | 现货 | ||
10 mg | ¥ 2,320 | 现货 | ||
25 mg | ¥ 3,830 | 现货 | ||
50 mg | ¥ 5,490 | 现货 | ||
100 mg | ¥ 7,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,380 | 现货 |
产品描述 | GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis. |
靶点活性 | HCA2 (hydroxy-carboxylic acid receptor 2):pEC50: 7.5 |
体外活性 | GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes. GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin). In membranes prepared from Chinese hamster ovary cells expressing recombinant human HCA2, It has good activity versus the rat orthologue of HCA2 (pEC50 value of 6.9 compared to 6.4 for niacin) [2]. |
体内活性 | GSK256073 (i.v.; 1-10 mg/kg) produces a dose-related decrease in NEFA, however, the enhanced in-ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin. GSK256073 (p.o.; 1, 30, and 100 mg/kg; in rat) displays that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Although the duration was longer with a reduction of 91% still present 6 h post-dose at 10 mg/kg, triglycerides reduce is followed as a similar pattern [2]. |
分子量 | 256.69 |
分子式 | C10H13ClN4O2 |
CAS No. | 862892-90-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16.67 mg/mL (64.94 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.8957 mL | 19.4787 mL | 38.9575 mL | 97.3937 mL |
5 mM | 0.7791 mL | 3.8957 mL | 7.7915 mL | 19.4787 mL | |
10 mM | 0.3896 mL | 1.9479 mL | 3.8957 mL | 9.7394 mL | |
20 mM | 0.1948 mL | 0.9739 mL | 1.9479 mL | 4.8697 mL | |
50 mM | 0.0779 mL | 0.3896 mL | 0.7791 mL | 1.9479 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK256073 862892-90-8 Endocrinology/Hormones GPCR/G Protein Others GPR type 2 Inhibitor mellitus GSK-256073 HM74A HCA2 homeostasis GPCR T2DM dyslipidaemia GSK 256073 glucose HCAR2 diabete inhibit GPR109A PUMA-G inhibitor