Liraglutide binds to the same receptors as does the endogenous metabolic hormone GLP-1. Liraglutide can be used to treat obesity in adults with some related comorbidity. Liraglutide activated AMPK/SREBP1 pathway in oxLDL-stimulated Raw264.7 cells.
|Cell lines||human umbilical vein endothelial cell line C11-STH20|
|Preparation method||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.|
|Incubation time||16 h|
|Animal models||Athymic nude mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||Water: ≥ 5 mg/mL|
|Storage||-20°C, protect from light, dry, sealed|
Liraglutide Compromises Pancreatic β Cell Function in a Humanized Mouse Model.
Abdulreda MH, et al. Cell Metab. 2016 Mar 8;23(3):541-6. PMID: 26876561.
Liraglutide reduces oxidized LDL-induced oxidative stress and fatty degeneration in Raw 264.7 cells involving the AMPK/SREBP1 pathway.
Wang YG, et al. J Geriatr Cardiol. 2015 Jul;12(4):410-6. PMID: 26346224.
A GLP-1 receptor agonist liraglutide inhibits endothelial cell dysfunction and vascular adhesion molecule expression in an ApoE-/- mouse model.
Gaspari T, et al. Diab Vasc Dis Res. 2011 Apr;8(2):117-24. PMID: 21562063.
|Related Glucagon Receptor Products|
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|Avexitide (Exendin 9-39)
Avexitide (Exendin 9-39) is a specific and competitive GLP-1 receptor antagonist.
Cotadutide acetate is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor, with EC50 values of 6.9 pM and 10.2 pM, respectively.
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