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抑制剂/激动剂
药物研究 囊泡
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G蛋白偶联受体/G蛋白
经典阳性药 小分子阳性药 帕金森与阿尔茨海默症
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Glucagon Receptor
糖尿病
/ Liraglutide

利拉鲁肽 /Liraglutide {[allProObj[0].p_purity_real_show]}

货号：A608103 同义名： 利拉糖肽 / NN 2211;Liraglutidum

Liraglutide是一种胰高血糖素样肽-1（GLP-1）受体激动剂，常用于2型糖尿病的临床治疗。

Liraglutide 化学结构 CAS号：204656-20-2
Liraglutide 化学结构
CAS号：204656-20-2
Liraglutide 3D分子结构
CAS号：204656-20-2
Liraglutide 化学结构 CAS号：204656-20-2
Liraglutide 3D分子结构 CAS号：204656-20-2
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Liraglutide 纯度/质量文件 产品仅供科研

货号：A608103 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]
• Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]
• ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]
• ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]
• Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]
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Liraglutide 生物活性

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.

Liraglutide 动物研究

Dose Mice: 0.057 mg/kg, 0.118 mg/kg[3] (i.p.), 0.3 mg/kg[4] (i.p.), 0.1 mg/kg - 1 mg/kg[5] (s.c.)
Rat: 0.1 mg/kg - 1 mg/kg[6] (s.c.)
Administration i.p., s.c.
Pharmacokinetics
Animal Mice[7] Rats[7] Monkeys[7]
Dose 0.1 mg/kg 0.1 mg/kg 0.12 mg/kg (i.v.)
0.05 mg/kg (s.c.)
Administration s.c. s.c. i.v.
s.c.
Vz 0.05 L/kg (i.v.)
T1/2 6.7 h 3.5 h 6.2 h (i.v.)
7.1 h (s.c.)
Tmax 6 h 6 h 7.3 h (s.c.)
CL 0.0055 L/h/kg (i.v.)
Cmax 750 nmol/L 770 nmol/L 600 nmol/L (s.c.)
Protein binding (free drug %) 99.5 - 99.7% 95.8 - 98.2%
Protein bound (%) 99.3 - 99.8%
AUC 11600 nmol·h/L 8700 nmol·h/L 49000 nmol·h/L (i.v.)
9700 nmol·h/L (s.c.)

Liraglutide 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 <<

Liraglutide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.27mL

0.05mL

0.03mL

1.33mL

0.27mL

0.13mL

2.67mL

0.53mL

0.27mL

Liraglutide 技术信息

CAS号204656-20-2
分子式C172H265N43O51
分子量 3751.2
别名 利拉糖肽 ;NN 2211;Liraglutidum;Saxenda, Victoza;NN 2211, NN-2211, NN2211;NNC 90-1170;Liraglutida
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
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
动物实验配方

Tags: Liraglutide | 204656-20-2 | GCGR | GLP Receptor | GLP-1R Agonist | GPCR/G Protein | GCGR | GLP Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Liraglutide 纯度/质量文件 | Liraglutide 生物活性 | Liraglutide 动物研究 | Liraglutide 临床数据 | Liraglutide 实验方案 | Liraglutide 技术信息

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