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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/利拉鲁肽 {[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/利拉鲁肽 化学结构 CAS号：204656-20-2
Liraglutide/利拉鲁肽 化学结构
CAS号：204656-20-2
Liraglutide/利拉鲁肽 3D分子结构
CAS号：204656-20-2
Liraglutide/利拉鲁肽 化学结构 CAS号：204656-20-2
Liraglutide/利拉鲁肽 3D分子结构 CAS号：204656-20-2
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Liraglutide/利拉鲁肽 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

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >

Liraglutide/利拉鲁肽 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/利拉鲁肽 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57BL6N mice Intraperitoneal injection 100 µg/kg Single injection, measurements taken at 2 and 4 hours post-injection To investigate the effects of liraglutide on bile acids and serotonin, results showed that liraglutide significantly decreased total bile acids and primary bile acids levels, and reduced serotonin levels in the colon. Int J Mol Sci. 2024 Jul 16;25(14):7784

Liraglutide/利拉鲁肽 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/利拉鲁肽 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/利拉鲁肽 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/利拉鲁肽 技术信息

CAS号204656-20-2
分子式C172H265N43O51
分子量 3751.2
SMILES Code NONE
MDL No. MFCD28126980
别名 利拉糖肽 ;NN 2211; Liraglutidum; Saxenda, Victoza; NN 2211, NN-2211, NN2211; NNC 90-1170; Liraglutida
运输蓝冰
InChI Key YSDQQAXHVYUZIW-QCIJIYAXSA-N
Pubchem ID 16134956
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
溶解方案

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

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/利拉鲁肽 纯度/质量文件 | Liraglutide/利拉鲁肽 生物活性 | Liraglutide/利拉鲁肽 动物研究 | Liraglutide/利拉鲁肽 临床数据 | Liraglutide/利拉鲁肽 实验方案 | Liraglutide/利拉鲁肽 技术信息

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