Liraglutide 是胰高血糖素样肽-1 受体激动剂，用于 2 型糖尿病的研究。

Liraglutide is a long-acting GLP-1 receptor agonist.

Liraglutide attenuates induction of plasminogen activator inhibitor type-1 (PAI-1) and vascular adhesion molecule (VAM) expression in human vascular endothelial cells (hVECs) in vitro and may afford protection against endothelial cell dysfunction (ECD), an early abnormality in diabetic vascular disease. In vitro studies demonstrates GLP-1R-dependent liraglutide-mediated inhibition of stimulated PAI-1 and VAM expression[3].

In vivo studies of vascular reactivity and immunohistochemical analysis are performed in the ApoE-/- mouse model. They demonstrate significant improvement in endothelial function in liraglutide treated mice, a GLP-1R dependent effect. Liraglutide treatment also increases endothelial nitric oxide synthase (eNOS) and reduces intercellular adhesion molecule-1 (ICAM-1) expression in aortic endothelium, an effect again dependent on the GLP-1R[3]. Liraglutide reduces hyperglycemia in T2D mouse models by increasing pancreatic b cell mass through enhanced proliferation[2].

Assay of ProRS activity: The prolyl tRNA synthetase domain of human EPRS (ProRS) is expressed in E.coli with a 6-his tag and purified. Enzymatic activity is assayed using incorporation of 3H Pro into the tRNA fraction essentially, except that the charged tRNA fraction is isolated by rapid batchwise binding to Mono Q sepharose and quantitated by liquid scintillation counting. For all kinetic assays, the concentration of active enzyme in the reaction is 40 nM. Similar inhibition by HF is seen using the human ProRS domain purified from bacteria and full length EPRS purified from rat liver.

C11-STH cells are cultured to confluence at 37°C in gelatin-coated Nunclon cell culture dishes in Media-199 supplemented with penicillin/streptomycin, 20% FCS, 20 μg/ml endothelial cell growth factor and 20 μg/ml heparin. C11-STH cells are incubated under serum free conditions with liraglutide (100 nM) or the GLP-1 receptor antagonist exendin (9-39) (100 nM) alone or with 10 ng/ml TNFα for 16 h alone or in combination with liraglutide and/or exendin (9-39). ELISA assays for VCAM-1 and ICAM-1 are performed using conditioned medium from C11-STH cells to determine protein expression levels.(Only for Reference)

204656-20-2

C172H265N43O51

3751.25

Liraglutidum;利拉糖肽;Victoza;Liraglutida;利拉鲁肽;NN2211

H2O:5 mg/mL (1.33 mM),ultrasonic and adjust pH to 8 with NaOH
Powder: -20°C for 3 years
In solvent: -80°C for 2 years