Liraglutide

Alias: NNC 90-1170; Liraglutide; NN 2211; NN-2211; NN2211; trade names: Saxenda; Victoza

Cat No.:V4643 Purity: = 98.76%

COA Product Data Instructions for use SDS

Liraglutide, a Glucagon-like Peptide 1 (GLP-1) analog, is a potent agonist of the Glucagon-like Peptide 1 receptor.

Liraglutide Chemical Structure CAS No.: 204656-20-2
Product category: GCGR

This product is for research use only, not for human use. We do not sell to patients.

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Major Universities, Research Institutions, Biotech & Pharma
Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: = 98.76%

COA

MSDS

HPLC

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Liraglutide, a Glucagon-like Peptide 1 (GLP-1) analog, is a potent agonist of the Glucagon-like Peptide 1 receptor. It is prescribed to patients with type 2 diabetes mellitus who do not respond to metformin as an anti-hyperglycemic agent and additional therapy.

Biological Activity I Assay Protocols (From Reference)

Targets	GLP-1 receptor
ln Vitro	Liraglutide may provide protection against endothelial cell dysfunction (ECD), an early abnormality in diabetic vascular disease, by attenuating the induction of plasminogen activator inhibitor type-1 (PAI-1) and vascular adhesion molecule (VAM) expression in human vascular endothelial cells (hVECs) in vitro. Research conducted in vitro indicates that stimulated expression of VAM and PAI-1 is inhibited by liraglutide in a GLP-1R-dependent manner[3].
ln Vivo	In the ApoE-/-mouse model, vascular reactivity and immunohistochemical analysis are investigated in vivo. In mice given liraglutide, they show a marked improvement in endothelial function, an effect that is dependent on GLP-1R. Additionally, ligandomycin treatment decreases the expression of intercellular adhesion molecule-1 (ICAM-1) in the aortic endothelium and increases endothelial nitric oxide synthase (eNOS), both of which are reliant on the GLP-1R[3]. Liraglutide increases pancreatic b cell mass through enhanced proliferation, which lowers hyperglycemia in T2D mouse models[2].
Cell Assay	In Nunclon cell culture dishes coated with gelatin and supplemented with Media-199 containing penicillin/streptomycin, 20% FCS, 20 µg/ml endothelial cell growth factor, and 20 µg/ml heparin, C11-STH cells are grown until confluence at 37°C. Under serum-free conditions, C11-STH cells are cultured with 100 nM liraglutide or 100 nM GLP-1 receptor antagonist exendin (9-39) alone, or with 10 ng/ml TNFα for 16 hours either in combination with liraglutide and/or exendin (9-39). Protein expression levels are measured using ELISA assays for VCAM-1 and ICAM-1 using conditioned medium from C11-STH cells.
Animal Protocol	Athymic nude mice 300 μg/kg/day s.c.
References	[1]. Am J Manag Care . 2011 Mar;17(2 Suppl):S59-70. [2]. Cell Metab . 2016 Mar 8;23(3):541-6. [3]. Diab Vasc Dis Res . 2011 Apr;8(2):117-24.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C172H265N43O51
Molecular Weight	3751.2020
Exact Mass	3748.95
Elemental Analysis	C, 55.07; H, 7.12; N, 16.06; O, 21.75
CAS #	204656-20-2
Related CAS #	Liraglutide-d8 triTFA; Liraglutide-13C5,15N tetraTFA
SequenceShortening	HAEGTFTSDVSSYL-{N6-[N-(1-oxohexadecyl)-L-γ-Etamyl]-Glu}-GQAAKEFIAWLVRGRG
Appearance	Solid powder
SMILES	CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC2=CNC3=CC=CC=C32)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)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC6=CN=CN6)N)C(=O)O
InChi Key	YSDQQAXHVYUZIW-QCIJIYAXSA-N
InChi Code	InChI=1S/C172H265N43O51/c1-18-20-21-22-23-24-25-26-27-28-29-30-37-53-129(224)195-116(170(265)266)59-64-128(223)180-68-41-40-50-111(153(248)199-115(62-67-135(232)233)154(249)204-120(73-100-44-33-31-34-45-100)159(254)214-140(93(11)19-2)167(262)192-97(15)146(241)201-122(76-103-79-183-108-49-39-38-48-106(103)108)157(252)203-118(72-90(5)6)158(253)212-138(91(7)8)165(260)200-110(52-43-70-182-172(177)178)149(244)184-81-130(225)193-109(51-42-69-181-171(175)176)148(243)187-84-137(236)237)196-144(239)95(13)189-143(238)94(12)191-152(247)114(58-63-127(174)222)194-131(226)82-185-151(246)113(61-66-134(230)231)198-155(250)117(71-89(3)4)202-156(251)119(75-102-54-56-105(221)57-55-102)205-162(257)124(85-216)208-164(259)126(87-218)209-166(261)139(92(9)10)213-161(256)123(78-136(234)235)206-163(258)125(86-217)210-169(264)142(99(17)220)215-160(255)121(74-101-46-35-32-36-47-101)207-168(263)141(98(16)219)211-132(227)83-186-150(245)112(60-65-133(228)229)197-145(240)96(14)190-147(242)107(173)77-104-80-179-88-188-104/h31-36,38-39,44-49,54-57,79-80,88-99,107,109-126,138-142,183,216-221H,18-30,37,40-43,50-53,58-78,81-87,173H2,1-17H3,(H2,174,222)(H,179,188)(H,180,223)(H,184,244)(H,185,246)(H,186,245)(H,187,243)(H,189,238)(H,190,242)(H,191,247)(H,192,262)(H,193,225)(H,194,226)(H,195,224)(H,196,239)(H,197,240)(H,198,250)(H,199,248)(H,200,260)(H,201,241)(H,202,251)(H,203,252)(H,204,249)(H,205,257)(H,206,258)(H,207,263)(H,208,259)(H,209,261)(H,210,264)(H,211,227)(H,212,253)(H,213,256)(H,214,254)(H,215,255)(H,228,229)(H,230,231)(H,232,233)(H,234,235)(H,236,237)(H,265,266)(H4,175,176,181)(H4,177,178,182)/t93-,94-,95-,96-,97-,98+,99+,107-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,138-,139-,140-,141-,142-/m0/s1
Chemical Name	(2S)-5-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-(hexadecanoylamino)-5-oxopentanoic acid
Synonyms	NNC 90-1170; Liraglutide; NN 2211; NN-2211; NN2211; trade names: Saxenda; Victoza
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ~100 mg/mL (~26.7 mM) Water: ~100 mg/mL Ethanol: ~100 mg/mL
Solubility (In Vivo)	5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 5.0mg/ml (1.33mM) (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

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Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
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In vivo Formulation Calculator (Clear solution)

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

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02516657	Active Recruiting	Drug: Liraglutide	Type 1 Diabetes	University at Buffalo	May 2012	Phase 3
NCT04529278	Active Recruiting	Drug: Liraglutide	Diabetes Mellitus, Type 2 Hemodialysis Obese	Fondation Hôpital Saint-Joseph	January 18, 2021	Phase 2
NCT04883346	Active Recruiting	Drug: Liraglutide	Obesity Status Post Sleeve Gastrectomy	Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	June 21, 2021	Phase 2
NCT02344186	Active Recruiting	Drug: Liraglutide	Type 2 Diabetes	Temple University	May 2014	Phase 4
NCT02944500	Active Recruiting	Drug: liraglutide Other: Placebo	Obesity	Beth Israel Deaconess Medical Center	November 2016	Phase 4

Biological Data

Effects of long-term daily liraglutide treatment on glucose homeostasis. Cell Metab . 2016 Mar 8;23(3):541-6.