Home>>Signaling Pathways>> GPCR/G protein>> Glucagon Receptor>>Liraglutide

Liraglutide (Synonyms: HAEGTFTSDVSSYL-{N6-[N-(1-oxohexadecyl)-L-γ-Etamyl]-Glu}-GQAAKEFIAWLVRGRG)

Catalog No.GC10311

Liraglutide is a highly potent, long-acting GLP-1 receptor agonist (EC50 = 61 pM)and shares 97% of its amino acid sequence identity with human GLP-1 .

Products are for research use only. Not for human use. We do not sell to patients.

Liraglutide Chemical Structure

Cas No.: 204656-20-2

Size Price Stock Qty
1mg
$102.00
In stock
5mg
$417.00
In stock
10mg
$748.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

Protocol

Kinase experiment [1]:

Preparation Method

A cloned human GLP-1 receptor expressed in juvenile hamster kidney (BHK) cells was used, Study on functional assays of compounds( Liraglutide ) using SAR.

Reaction Conditions

10-14 -10-5 M liraglutide

Applications

Liraglutide is a highly potent, long-acting GLP-1 receptor agonistand and shares 97% of its amino acid sequence identity with human GLP-1 (EC50 = 61 pM).

Cell experiment [2]:

Cell experiment

HepG2 cell line

Preparation Method

Cell viability assay :HepG2 cells were seeded onto a 96-well plate, then treated with PA and LPS in the presence of liraglutide (0, 50, 100, 200, 500 nM) for 16 h. The number of viable cells was determined using Cell Counting Kit-8 (CCK-8)

Reaction Conditions

liraglutide (0, 50, 100, 200, 500 nM) for 16 h

Applications

The number of viable cells in hepatocytes treated with PA/LPS was significantly reduced, and liraglutide reversed the decline in cell viability in a concentration-dependent manner. Liraglutide at 100 nM significantly increased cell viability compared with higher concentrations.

Animal experiment [3]:

Animal models

Male ApoE KO mice on C57BL/6 background

Preparation Method

Liraglutide (1 mg/kg) or saline was given intraperitoneally twice daily for 8 weeks (from 9th to 16th week of HFD feeding)

Dosage form

Liraglutide (1 mg/kg) for 8 weeks

Applications

Liraglutide treatment improved insulin sensitivity and increased Acrp30 plasma levels and transcriptional activity, Liraglutide treatment reduces liver fat content, Liraglutide was sufficient to protect mice from the inflammatory consequences of HFD and Acrp30 knockdown.

References:

[1]. Knudsen LB, Nielsen PF,et,al. Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. J Med Chem. 2000 May 4;43(9):1664-9. doi: 10.1021/jm9909645. PMID: 10794683

[2]. Yu X, Hao M, et,al. Liraglutide ameliorates non-alcoholic steatohepatitis by inhibiting NLRP3 inflammasome and pyroptosis activation via mitophagy. Eur J Pharmacol. 2019 Dec 1;864:172715. doi: 10.1016/j.ejphar.2019.172715. Epub 2019 Oct 5. PMID: 31593687.

[3]. Zhang L, Yang M, et,al. GLP-1 analogue prevents NAFLD in ApoE KO mice with diet and Acrp30 knockdown by inhibiting c-JNK. Liver Int. 2013 May;33(5):794-804. doi: 10.1111/liv.12120. Epub 2013 Feb 24. PMID: 23432843.

Background

Liraglutide is a highly potent, long-acting GLP-1 receptor agonist (EC50 = 61 pM)and shares 97% of its amino acid sequence identity with human GLP-1 [6,7].

The number of viable cells in hepatocytes treated with PA/LPS was significantly reduced, and liraglutide reversed the decline in cell viability in a concentration-dependent manner. Liraglutide at 100 nM significantly increased cell viability compared with higher concentrations[1].In H9c2 cardiomyoblasts,Pretreatment with 100 nM liraglutide could efficiently inhibit TNF-α and hypoxia-induced inflammasome activation. liraglutide reversed the level of SIRT1,Liraglutide diminished the levels of ROS generation and NOX4 expression[2]. Liraglutide relieved steatosis by improving hepatic fat synthesis, transportation, storage, and use via PI3K and AMPK pathways [3].The cytoplasmic lipid droplet accumulation was visibly decreased in foam cells by treatment with liraglutide. The TG and cholesterol content in the liraglutide-treated foam cells was significantly decreased. Expression level of AMPKα1 and phosphorylated AMPKα1 was significantly increased while the expression level of SREBP1 and phosphorylated SREBP1 was significantly decreased in foam cells following treatment with liraglutide[5].

In mice,The combination of HFD, Acrp30 knockdown and ApoE deficiency had additive effects on the development of insulin resistance (IR) and NAFLD. Administration of liraglutide prevented the development of HFD and hypoadiponectinaemia-induced IR and NAFLD in this model. Liraglutide also attenuated the expression of proinflammatory cytokines or transcription factor, including TNF-α and NF-κB(65) , and the expression of two lipogenesis-related genes, Acetyl-CoA Carboxylase (ACC) and fatty acid synthase (FAS)[4].

References:
[1]: Yu X, Hao M, et,al. Liraglutide ameliorates non-alcoholic steatohepatitis by inhibiting NLRP3 inflammasome and pyroptosis activation via mitophagy. Eur J Pharmacol. 2019 Dec 1;864:172715. doi: 10.1016/j.ejphar.2019.172715. Epub 2019 Oct 5. PMID: 31593687.
[2]: Chen A, Chen Z, et,al. Liraglutide attenuates NLRP3 inflammasome-dependent pyroptosis via regulating SIRT1/NOX4/ROS pathway in H9c2 cells. Biochem Biophys Res Commun. 2018 May 5;499(2):267-272. doi: 10.1016/j.bbrc.2018.03.142. Epub 2018 Mar 23. PMID: 29571736.
[3]: Liu J, Wang G, et,al. GLP-1 receptor agonists: effects on the progression of non-alcoholic fatty liver disease. Diabetes Metab Res Rev. 2015 May;31(4):329-35. doi: 10.1002/dmrr.2580. Epub 2014 Sep 14. PMID: 25066109.
[4]: Zhang L, Yang M, et,al. GLP-1 analogue prevents NAFLD in ApoE KO mice with diet and Acrp30 knockdown by inhibiting c-JNK. Liver Int. 2013 May;33(5):794-804. doi: 10.1111/liv.12120. Epub 2013 Feb 24. PMID: 23432843.
[5]: Wang YG, Yang TL. Liraglutide reduces oxidized LDL-induced oxidative stress and fatty degeneration in Raw 264.7 cells involving the AMPK/SREBP1 pathway. J Geriatr Cardiol. 2015 Jul;12(4):410-6. doi: 10.11909/j.issn.1671-5411.2015.04.013. PMID: 26346224; PMCID: PMC4554794.
[6]: Bode B. Liraglutide: a review of the first once-daily GLP-1 receptor agonist. Am J Manag Care. 2011 Mar;17(2 Suppl):S59-70. PMID: 21517658.
[7]: Knudsen LB, Nielsen PF, et,al. Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. J Med Chem. 2000 May 4;43(9):1664-9. doi: 10.1021/jm9909645. PMID: 10794683.

Chemical Properties

Cas No. 204656-20-2 SDF
Synonyms HAEGTFTSDVSSYL-{N6-[N-(1-oxohexadecyl)-L-γ-Etamyl]-Glu}-GQAAKEFIAWLVRGRG
Canonical 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(
Formula C172H265N43O51 M.Wt 3751.2
Solubility <20mg/mL in Water, ≥ 3.85mg/mL in Acetic acid:Water:DMSO=1:1:1 Storage Store at -20°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 0.2666 mL 1.3329 mL 2.6658 mL
5 mM 0.0533 mL 0.2666 mL 0.5332 mL
10 mM 0.0267 mL 0.1333 mL 0.2666 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

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 as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Liraglutide

Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Liraglutide

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.