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Liraglutide Glp-1 Receptor agonist

Cat.No.S8256

Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist.
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Quality Control

Batch: Purity: 99.84%
99.84

Cell Culture, Treatment & Working Concentration

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
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Solubility

In vitro
Batch:

DMSO : 100 mg/mL (26.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

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

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

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Mechanism of Action

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

Applications

Methods Biomarkers Images PMID
Western blot p-ERK / p-JNK / p-p38 / p-AKT / IκB-α
S8256-WB1
24217090

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-05-29)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06742710 RECRUITING
PCOS; Obesity; Infertility
Peking University Third Hospital
2025-05-22 PHASE4
NCT06976619 RECRUITING
Type 1 Diabetes; Type 2 Diabetes
Mayo Clinic
2025-10-03 PHASE2
NCT05681299 RECRUITING
Healthy; Growth Hormone Deficiency
Columbia University
2023-05-01 PHASE4
NCT07244003 RECRUITING
T2DM (Type 2 Diabetes Mellitus)
Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.
2025-03-29 PHASE4
NCT07301437 NOT_YET_RECRUITING
Overweight and Obese Adults
The Fourth Affiliated Hospital of Zhejiang University School of Medicine
2026-05-01 PHASE4
NCT06171152 SUSPENDED
Multiple Sclerosis; Long COVID; Long Covid19; Obese; Obesity; Obesity, Morbid; Acute Leukemia in Remission
University of Chicago
2024-01-26 EARLY_PHASE1

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