Liraglutide (CAS: 204656-20-2)

C₁₇₂H₂₆₅N₄₃O₅₁

• Long-acting acylated glucagon-like peptide-1 (GLP-1) receptor agonist.
• Antidiabetic and antiobesity agent used clinically to treat type 2 diabetes mellitus. Binding to GLP-1R, activates AMP-activated protein kinase, consequently stimulates insulin secretion in pancreatic β cells and suppresses glucagon secretion in a glucose-dependent manner. Improves control of blood glucose and consequently modulates appetite and body weight.
• Inhibits β cell apoptosis and improves β cell mass.
• Shown to ameliorate glycometabolism and insulin resistance through the upregulation of GLUT4.
• Neuroprotective. Prevents neurodegenerative processes in pathologies such as Alzheimer's and Parkinson's disease.
• Anti-inflammatory agent. Exerts cardioprotective roles via activating prosurvival pathways and suppressing inflammation. Anti-pyroptotic by inhibiting TNF-α and hypoxia-induced inflammasome activation.
• Anticancer agent. Inhibited proliferation and induced apoptosis in cancer cell lines.
• Shown to inhibit osteoclastogenesis.

1. The pharmacokinetics, pharmacodynamics, safety and tolerability of NN2211, a new long-acting GLP-1 derivative, in healthy men: H. Agerso, et al.; Diabetologia 45, 195 (2002)
2. The long-acting GLP-1 derivative NN2211 ameliorates glycemia and increases beta-cell mass in diabetic mice: B. Rolin, et al.; Am. J. Physiol. Endocrinol. Metab. 283, E745 (2002)
3. The long-acting glucagon-like peptide-1 analogue, liraglutide, inhibits beta-cell apoptosis in vitro: S. Bregenholt, et al.; BBRC 330, 577 (2005)
4. Pharmacokinetics and pharmacodynamics of liraglutide, a long-acting, potent glucagon-like peptide-1 analog: J. Meece; Pharmacotherapy 29, 33S (2009) (Review)
5. The diabetes drug liraglutide prevents degenerative processes in a mouse model of Alzheimer's disease: P.L. McClean, et al.; J. Neurosci. 31, 6587 (2011)
6. Potential role of glucagon-like peptide-1 (GLP-1) in neuroprotection: C. Hoelscher; CNS Drugs 26, 871 (2012) (Review)
7. Liraglutide ameliorates glycometabolism and insulin resistance through the upregulation of GLUT4 in diabetic KKAy mice: L.N. Chen, et al.; Int. J. Mol. Med. 32, 892 (2013)
8. Liraglutide can reverse memory impairment, synaptic loss and reduce plaque load in aged APP/PS1 mice, a model of Alzheimer's disease: P.L. McClean & C. Hoelscher; Neuropharmacol. 76, 57 (2014)
9. Glucagon-like peptide-1 (GLP-1) analog liraglutide inhibits endothelial cell inflammation through a calcium and AMPK dependent mechanism: N.M. Krasner, et al.; PLoS One 9, e97554 (2014)
10. Liraglutide acutely suppresses glucagon, lipolysis and ketogenesis in type 1 diabetes: M. Garg, et al.; Diabetes Obes. Metab. 19, 1306 (2017)
11. Liraglutide, a glucagon-like peptide-1 analog, induce autophagy and senescence in HepG2 cells: G.C. Krause, et al.; Eur. J. Pharmacol. 809, 32 (2017)
12. Liraglutide inhibits the proliferation and promotes the apoptosis of MCF-7 human breast cancer cells through downregulation of microRNA-27a expression: W. Zhao, et al.; Mol. Med. Rep. 17, 5202 (2018)
13. Liraglutide attenuates NLRP3 inflammasome-dependent pyroptosis via regulating SIRT1/NOX4/ROS pathway in H9c2 cells: A. Chen, et al.; BBRC 499, 267 (2018)
14. Liraglutide Modulates Appetite and Body Weight Via GLP-1R-Expressing Glutamatergic Neurons: J.M. Adams, et al.; Diabetes (Epub ahead of print) (2018)
15. Liraglutide exerts a bone-protective effect in ovariectomized rats with streptozotocin-induced diabetes by inhibiting osteoclastogenesis: B. Wen, et al.; Exp. Ther. Med. 15, 5077 (2018)