Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Anagliptin (SK-0403) 是一种选择性的二肽酰肽酶 4 抑制剂,IC50=3.8 nM,对 DPP-8/9 的选择性相对较弱,IC50分别为 68 和 60 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 462 | 现货 | ||
5 mg | ¥ 955 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 2,950 | 现货 | ||
50 mg | ¥ 4,970 | 现货 | ||
100 mg | ¥ 6,860 | 现货 | ||
500 mg | ¥ 13,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,050 | 现货 |
产品描述 | Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus. |
靶点活性 | DPP8:68 nM , DPP9:60 nM, DPP4:3.8 nM |
体外活性 | Soluble DPP-4 augmented cultured SMC proliferation, and anagliptin suppressed the proliferation by inhibiting ERK phosphorylation.?In THP-1 cells, anagliptin reduced lipopolysaccharide-induced TNF-α production with inhibiting ERK phosphorylation and nuclear translocation of nuclear factor-κB.?Quantitative analysis also showed that anagliptin reduced the area of atherosclerotic lesion in apoE-deficient mice[1]. |
体内活性 | Treatment with anagliptin for 16 wk significantly reduced accumulation of monocytes and macrophages in the vascular wall, SMC content in plaque areas, and oil red O-stained area around the aortic valve without affecting glucose tolerance or body weight.?Serum DPP-4 concentrations were significantly higher in apoE-deficient mice than control mice, and the levels increased with aging, suggesting the involvement of DPP-4 in the progression of atherosclerosis[1]. Anagliptin treatment significantly decreased the plasma total cholesterol (14% reduction, P < 0.01) and triglyceride levels (27% reduction, P < 0.01). Both low-density lipoprotein cholesterol and very low-density lipoprotein cholesterol were also decreased significantly by anagliptin treatment. Sterol regulatory element-binding protein-2 messenger ribonucleic acid expression level was significantly decreased at night in anagliptin-treated mice (15% reduction, P < 0.05). Anagliptin significantly suppressed sterol regulatory element-binding protein activity in HepG2 cells (21% decrease, P < 0.001)[2]. |
动物实验 | Male low-density lipoprotein receptor-deficient mice were administered 0.3% anagliptin in their diet.?Plasma lipid levels were assayed and lipoprotein profile was analyzed using high-performance liquid chromatography.?Hepatic gene expression was examined by deoxyribonucleic acid microarray and quantitative polymerase chain reaction analyses[2]. |
别名 | SK-0403, 阿拉格列汀 |
分子量 | 383.45 |
分子式 | C19H25N7O2 |
CAS No. | 739366-20-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (130.4 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6079 mL | 13.0395 mL | 26.079 mL | 65.1975 mL |
5 mM | 0.5216 mL | 2.6079 mL | 5.2158 mL | 13.0395 mL | |
10 mM | 0.2608 mL | 1.304 mL | 2.6079 mL | 6.5198 mL | |
20 mM | 0.1304 mL | 0.652 mL | 1.304 mL | 3.2599 mL | |
50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.304 mL | |
100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.652 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。
Anagliptin 739366-20-2 Proteases/Proteasome Ubiquitination Proteasome DPP-4 lipid‐lowering smooth muscle cell inhibit Dipeptidyl Peptidase SK-0403 DPP SK 0403 DPP-8 SMC SK0403 atherosclerosis Inhibitor 阿拉格列汀 inhibitor