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Liraglutide

Name: Liraglutide
Brand: Selleck Chemicals
SKU: S8256
Rating: 5 (21 reviews)

Synonyms: NN2211, Liraglutida, Liraglutidum

Catalog No.S8256 Purity:99.84%

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

Liraglutide Chemical Structure

CAS No. 204656-20-2

Purity & Quality Control

Batch: Purity: 99.84%

99.84

Liraglutide Related Products

Related Targets	GLP-1R GL-R	Click to Expand
Related Products	Relacorilant (CORT125134)	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ GPCR Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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

Biological Activity

Description

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

Targets

GLP-1 receptor ^[1]

In vitro
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 liraglutide-mediated inhibition of stimulated PAI-1 and VAM expression^[3].
Cell Research	Cell lines	human umbilical vein endothelial cell line C11-STH20
	Concentrations	100 nM
	Incubation Time	16 h
	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	p-ERK / p-JNK / p-p38 / p-AKT / IκB-α		24217090

In Vivo
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. Liraglutide 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^[3]. Liraglutide reduces hyperglycemia in T2D mouse models by increasing pancreatic b cell mass through enhanced proliferation^[2].
Animal Research	Animal Models	Athymic nude mice
	Dosages	300 μg/kg/day
	Administration	s.c.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

Chemical Information & Solubility

Molecular Weight	3751.25	Formula	C₁₇₂H₂₆₅N₄₃O₅₁
CAS No.	204656-20-2	SDF	Download Liraglutide SDF Download Liraglutide SDF
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
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (26.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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