Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DC260126 是一种 GPR40 (FFAR1)拮抗剂,对棕榈酸酯诱导的内质网应激和凋亡有保护作用。它剂量依赖性地抑制亚油酸、油酸、棕榈油酸和月桂酸刺激的 GPR40 介导的 Ca2+升高,IC50分别 6.28、5.96、7.07和4.58 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 415 | 现货 | ||
10 mg | ¥ 581 | 现货 | ||
25 mg | ¥ 1,255 | 现货 | ||
50 mg | ¥ 1,992 | 现货 | ||
100 mg | ¥ 3,629 | 现货 |
产品描述 | DC260126 is a small-molecule antagonist of FFA1 (GPR40) |
体内活性 | DC260126, a small molecule antagonist of GPR40, on β-cell function following administration of 10 mg/kg dose of DC260126 to obese diabetic db/db mice. Oral glucose tolerance test, glucose stimulated insulin secretion and insulin tolerance test were used to investigate the pharmacological effects of DC260126 on db/db mice after 21-days treatment. Immunohistochemistry and serum biochemical analysis were also performed. Although no significant change of blood glucose levels was found in DC260126-treated mice, DC260126 significantly inhibited glucose stimulated insulin secretion, reduced blood insulin level and improved insulin sensitivity after 3 weeks administration in db/db mice. Moreover, DC260126 reduced the proinsulin/insulin ratio and the apoptotic rate of pancreatic β-cells remarkably in DC260126-treated db/db mice compared to vehicle-treated mice (p<0.05, n = 8). Suggest that although DC260126 could not provide benefit for improving hyperglycemia, it could protect against pancreatic β-cells dysfunction through reducing overload of β-cells, and it increases insulin sensitivity possibly via alleviation of hyperinsulinemia in db/db mice[1]. |
动物实验 | To investigate the dose-dependent effect of DC260126, nine-week-old db/db male mice were divided into four groups (n = 6/group). Mice were give vehicle (5% DMSO in PBS) or DC260126 (3, 10, 30 mg/kg) once daily by tail vein injection for 5 days. At day 5, each group of mice were fasted for 6 h and blood samples were collected from orbital venous plexus and centrifuged for serum separation. Then the concentration of serum insulin level was measured by ELISA kit following its protocol. For long term experiments, six-week-old obese db/db male mice were divided into two groups (n = 8/group) and given vehicle (5% DMSO in PBS) or DC260126 (10 mg/kg) once daily by tail vein injection for 24 days, respectively. Meanwhile, their lean littermates were treated with vehicle in an identical manner as normal control. Body weight and food intake were recorded regularly. After 6 h fasting, blood glucose concentrations were monitored by tail vein blood using a glucometer every week. At the end of the experiment, mice were fasted for 12 h to perform oral glucose tolerance test (OGTT, day 21) and for 6 h to generate insulin tolerance test (ITT, day 23) as described with slight modification indicated . Meanwhile, the insulin release during OGTT was also measured, blood sample was obtained from tail veins and serum insulin concentration was determined by ELISA kit (Alpco, USA). At the end of experiment (day 24), mice were fasted for 6 h, and blood samples were collected from orbital venous plexus and centrifuged for serum separation. Then the animals were killed by CO2 inhalation, the pancreas tissue were removed and kept in 4% paraformaldehyde[1]. |
分子量 | 307.38 |
分子式 | C16H18FNO2S |
CAS No. | 346692-04-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (325.33 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2533 mL | 16.2665 mL | 32.533 mL | 81.3326 mL |
5 mM | 0.6507 mL | 3.2533 mL | 6.5066 mL | 16.2665 mL | |
10 mM | 0.3253 mL | 1.6267 mL | 3.2533 mL | 8.1333 mL | |
20 mM | 0.1627 mL | 0.8133 mL | 1.6267 mL | 4.0666 mL | |
50 mM | 0.0651 mL | 0.3253 mL | 0.6507 mL | 1.6267 mL | |
100 mM | 0.0325 mL | 0.1627 mL | 0.3253 mL | 0.8133 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。
DC260126 346692-04-4 Apoptosis Endocrinology/Hormones GPCR/G Protein GPR stress FFAR DC 260126 Inhibitor insulin inhibit secretion Free Fatty Acid Receptor DC-260126 phosphorylation elevation Ca2+ inhibitor