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Cat.No.S8256
| Related Targets | K-Ras CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras |
|---|---|
| Other GLP-1 Receptor Products | Danuglipron (PF-06882961) Exenatide (Exendin-4) Acetate ECC5004(AZD5004) |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| HepG2 | Proliferation assay | 0, 1, 10, 100, and 1000 nmol/L | 48 h | IC50~100 nM | 31081108 | |
| MiaPaca-2 | Cell viability assay | 0, 10, 100, 1000 nM | 48 h | The inhibitory effects on cell viability and cell number were statistically significant only at the concentration of 1,000 nmol/L for liraglutide | 29897998 | |
| H9c2 | Function assay | 100 nM | 1 h | Liraglutide reversed the downregulation of SIRT1 induced by TNF-α and hypoxia | 29571736 | |
| MC3T3-E1 | Apoptosis assay | 0, 10, 100, or 1000 nM | 48 h | liraglutide suppressed the apoptosis of MC3T3-E1 cells | 29463067 | |
| MCF-7 | Proliferation assay | 10, 100, 1,000 and 10,000 nM | 48 h | Liraglutide inhibits the proliferation and promotes apoptosis in the MCF-7 breast cancer cell line | 29393459 | |
| SH-SY5Y | Function assay | 100 nM | 16 h | Liraglutide resolves UPR in the neuroblastoma SH-SY5Y cell line. | 29170452 | |
| HEK293 | Function assay | up to 30 mins | Agonist activity at human GLP1 receptor expressed in HEK293 cells harboring mCerulean and mCitrine fused Epac protein assessed as increase in cAMP level up to 30 mins by fluorescence assay, EC50 = 0.000067 μM. | 28771355 | ||
| HEK293 | Function assay | 30 mins | Agonist activity at human GLP1 receptor expressed in HEK293 cells assessed as increase in cAMP level after 30 mins by HTRF method, EC50 = 0.0074 μM. | ChEMBL | ||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 100 mg/mL
(26.65 mM)
Water : 100 mg/mL Ethanol : 100 mg/mL |
|
In vivo |
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| Molecular Weight | 3751.25 | Formula | C172H265N43O51 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 204656-20-2 | Download SDF Download SDF | Storage of Stock Solutions |
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| Synonyms | NN2211, Liraglutida, Liraglutidum | Smiles | CCCCCCCCCCCCCCCC(=O)NC(CCC(=O)NCCCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)CC)C(=O)NC(C)C(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCNC(=N)N)C(=O)NCC(=O)NC(CCCNC(=N)N)C(=O)NCC(=O)O)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCC(=O)N)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CO)NC(=O)C(C(C)C)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C(CC6=CN=CN6)N)C(=O)O | ||
| Targets/IC50/Ki |
GLP-1 receptor
|
|---|---|
| In vitro |
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 this compound-mediated inhibition of stimulated PAI-1 and VAM expression. |
| In vivo |
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. This compound 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. It reduces hyperglycemia in T2D mouse models by increasing pancreatic b cell mass through enhanced proliferation. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | p-ERK / p-JNK / p-p38 / p-AKT / IκB-α |
|
24217090 |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06283641 | Enrolling by invitation | Obesity |
Novo Nordisk A/S |
February 23 2024 | -- |
| NCT05268237 | Recruiting | Diabete Type 2 |
Biolingus|Chinese University of Hong Kong |
April 25 2023 | Phase 1|Phase 2 |
| NCT05419856 | Completed | Knee Osteoarthritis |
4Moving Biotech|4P-Pharma |
August 9 2022 | Phase 1 |
| NCT05467514 | Completed | Diabetes Mellitus Type 1 |
David Sanchez Garcia|Instituto Mexicano del Seguro Social |
July 1 2022 | Phase 3 |
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