Liraglutide
产品说明书
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同义名 : | 利拉糖肽 ;NN 2211;Liraglutidum;Saxenda, Victoza;NN 2211, NN-2211, NN2211;NNC 90-1170;Liraglutida |
| CAS号 : | 204656-20-2 | |
| 货号 : | A608103 | |
| 分子式 : | C172H265N43O51 | |
| 纯度 : | 99% | |
| 分子量 : | 3751.2 | |
| MDL号 : | MFCD28126980 | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 5 mg/mL(1.33 mM)，配合低频超声，水浴加热至45℃，并调节pH至4 0.1 M NaOH: 10 mg/mL(2.67 mM)，调节pH至8 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The glucagon-like peptide-1(GLP-1) can potentiate β cell response to glucose for its important role in glucose-stimulated insulin release and thus been frequently used in type 2 diabetes (T2D) clinical therapy. Liraglutide is a potent, long-acting GLP-1 receptor agonist with EC50 value of 61pM, which is usually given , s.c., once daily with the average half-life of 12 hours. In hVEC and C11-STH cells, Liraglutide mediated inhibition of TNFα independent of PKA signaling. Treatment of mice model at 80nM/kg of this drug twice a day for 4 weeks demonstrated a significant improvement in endothelial function with max relaxation of 78.45%. Besides, expression of eNOS in the mice was also significantly increased and the ICAM-1 expression was inhibitedin vivo, suggesting GLP-1R signalling events of Liraglutide mediated by non-PKA . Also in diabetic mice model transplanted with human islets, treatment of them daily with liraglutide (300 μg/kg) showed enhanced initial function of the transplanted human islets without adverse systemic side effects. No additional improvement of the islets was found when the treatment last for >200 days. The lower Human C-peptide plasma levels and slower kinetics of insulin release from the human islets were also observed. When the time last for >240 days, peripheral insulin sensitivity was decreased, suggesting the association between hormone release from the β-cell and long-term treatment with this drug. Meanwhile, the concentration at which the cell apoptosis was increased by direct cytotoxic effects on the β-cell was higher. In a clinical study, 49 T2D patients treated with Liraglutide therapy showed 19% increasing of Mean glucose levels as well as 7% increasing of Mean postprandial glucose levels on Day 1. Meanwhile, the mean body weights of these patients decreased by -3.53kg while the lean body mass, % body fat decreased by -0.47 and -0.37 respectively, suggesting the reduction of timing limitation for liraglutide used in healthcare patients. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02138045 | Diabetes Mellitus, Type 1 ... 展开 >> Type 1 Diabetes Mellitus 收起 << | Not Applicable | Unknown | February 2017 | Denmark ... 展开 >> Mech-Sense, Department of Medical Gastroenterology, Aalborg University Hospital Aalborg, Jutland, Denmark, 9000 收起 << |
| NCT02014740 | - | Completed | - | - | |
| NCT01911468 | PCOS Obesity | Phase 4 | Completed | - | Slovenia ... 展开 >> University Medical Center Ljubljana Ljubljana, Slovenia, 1000 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
0.27mL 0.05mL 0.03mL |
1.33mL 0.27mL 0.13mL |
2.67mL 0.53mL 0.27mL |
