Liraglutide

SKU: orb1300385

Description

Liraglutide is a synthetic GLP-1 receptor agonist used in research for type 2 diabetes and obesity. It is widely applied in both in vitro binding assays and in vivo metabolic studies to investigate mechanisms of glucose homeostasis and weight regulation.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 204656-20-2
• MW: 3751.25
• Purity: 99.04% (May vary between batches)
• Formula: C₁₇₂H₂₆₅N₄₃O₅₁
• SMILES: CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)C(O)=O
• Target: Glucagon Receptor
• Solubility: H2O:5 mg/mL (1.33 mM)

Bioactivity

• Target IC50:
  HEK293 cells (GLP-1 receptor expressed):65.7 pM (EC50)|LPS-induced production of PEG2:54 nM|GLP1:542.4 ± 187.5 nM|HEK293 cells (GLP1 receptor overexpressed):9.3 pM (EC50)|LPS-induced production of NO:45 nM|GLP1 receptor:0.11 nM
• In Vivo:
  METHODS: To investigate the effects on diabetes, Liraglutide (100 µg/kg) was administered intraperitoneally once daily for two weeks to a BKS mouse model of type 2 diabetes. RESULTS: Liraglutide restored islet size, reduced islet β-cell apoptosis, and improved nephrin expression, a protein involved in β-cell survival signaling.Liraglutide protected βTC-6 cells from serum withdrawal-induced apoptosis by inhibiting caspase-3 activation.
• In Vitro:
  METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Liraglutide (5-20 µM) for 48 h. Cell viability was measured by direct cell counting. RESULTS: Incubation for 48 h with 15 µM and 20 µM of Liraglutide resulted in a significant decrease in cell proliferation compared to the control. METHODS: Pancreatic βTC-6 cells were treated with Liraglutide (1 nM) for 3-30 min, and the expression levels of target proteins were detected by Western Blot. RESULTS: Treatment of cells with Liraglutide resulted in an increase in phosphorylation of the pro-survival kinase AKT at Ser47 3 over time compared to untreated cells.
• Cell Research:
  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)

Storage & Handling

• Storage: keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NN2211, NN-2211, NN 2211, inhibit, Liraglutida, Liraglutide, Liraglutidum, Inhibitor, GCGR, GlucagonReceptor, Glucagon Receptor, GLP-1, Victoza

Compound Identifiers

PubChem CID

16134956