Lixisenatide

Alias: Lyxumia; Adlyxin; ZP10A peptide; ZP10 A peptide; ZP10-A peptide; AVE-0010; AVE0010; AVE 0010

Cat No.:V2751 Purity: ≥98%

COA Product Data Instructions for use SDS

Lixisenatide (ZP10A; ZP-10A; AVE-0010; AVE0010; Lyxumia, Adlyxin) is a short-acting agonist of the glucagon-like peptide-1 receptor (GLP-1R) with anti-diabetic effects.

Lixisenatide Chemical Structure CAS No.: 320367-13-3
Product category: GCGR

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

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1-708-310-1919 sales@invivochem.com

Other Forms of Lixisenatide:

Lixisenatide acetate

Official Supplier of:

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%

COA

MSDS

Instructions

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

Product Description

Lixisenatide (ZP10A; ZP-10A; AVE-0010; AVE0010; Lyxumia, Adlyxin) is a short-acting agonist of the glucagon-like peptide-1 receptor (GLP-1R) with anti-diabetic effects. In in vitro receptor binding experiments, it activates GLP-1R with an IC50 value of 1.4 nM. In 2016, lixisenatide received approval to treat type 2 diabetes mellitus (T2DM). It can be taken on a once-daily schedule. Lixisenatide has the ability to prevent apoptosis caused by lipids and cytokines in Ins-1 cells, a β-cell line derived from rats. More significantly, lixisenatide can maintain insulin synthesis, storage, and pancreatic β-cell function in vitro and prevent lipotoxicity-induced insulin depletion in human islets.

Biological Activity I Assay Protocols (From Reference)

Targets

MEK1; MEK2; MMP13; MMP-1; MMP-3

ln Vitro

In vitro activity: Lixisenatide inhibits apoptosis induced by lipids and cytokines in Ins-1 cells, a β-cell line derived from rats. More significantly, lixisenatide also maintains insulin synthesis, storage, and pancreatic β-cell function in vitro and inhibits lipotoxicity-induced insulin depletion in human islets. Lixisenatide is a very potent and selective GLP-1 receptor agonist, as demonstrated by binding studies in CHO-K1 cells overexpressing the human GLP-1 receptor. Its binding affinity (Ki = 1.33 ± 0.22 nM) is approximately 4-times greater than that of human GLP-1 (Ki = 5.09 ± 1.19 nM). Lixisenatide's high selectivity for the GLP-1 receptor is confirmed by the lack of any meaningful interactions with other possible pharmacological targets in more than 80 different binding assays[3].

ln Vivo

Compared to liraglutide and albiglutide, which are long-acting GLP-1-based peptides, lixisenatide is a short-acting GLP-1-receptor agonist with a half-life of 2-4 hours. Insulin release that is stimulated by glucose can be markedly enhanced by lixisenatide. When administered subcutaneously, lixisenatide reduces plasma glucose levels in healthy normoglycemic dogs in a dose-dependent manner following an oral glucose challenge. It also significantly lowers postprandial glucose excursions, as evidenced by a 67% reduction when compared to a placebo, without contributing to an increase in insulin concentrations. Lixisenatide's impact on dogs' postprandial blood glucose excursions is thought to be partly caused by delayed intestinal glucose absorption and inhibition of stomach emptying. In the db/db mouse and ZDF rat, dose-dependent decreases in plasma glucose following an oral glucose challenge have also been shown. Crucially, at physiological glucose concentrations, this activity is insensitive to glucose and is glucose-dependent. Chronic lixisenatide administration in db/db mice is associated with significant dose-dependent reductions in glycosylated hemoglobin (HbA1c) and prevents the progressive deterioration in glucose tolerance observed in control animals. For a duration of 12 weeks, lixisenatide 50 μg/kg/day subcutaneous infusion significantly lowers basal blood glucose and enhances oral glucose tolerance in ZDF rats when compared to control animals. In rats with normoglycemia, it has no hypoglycemic effect and has no effect on HbA1c. By promoting islet cell proliferation and neogenesis and inhibiting islet cell apoptosis, lixisenatide can preserve beta cell mass and function[1]. In diabetic animals, lixisenatide maintains pancreatic responsiveness[3].

Enzyme Assay

Lixisenatide, shown in in vitro receptor binding studies, is a short-acting agonist of the glucagon-like peptide-1 receptor (GLP-1R), with an IC50 value of 1.4 nM for the human GLP-1 receptor. One daily regimen can be used to administer it.

Cell Assay

Lixisenatide has the ability to prevent apoptosis caused by lipids and cytokines in Ins-1 cells, a β-cell line derived from rats. More significantly, lixisenatide can maintain insulin synthesis, storage, and pancreatic β-cell function in vitro and prevent lipotoxicity-induced insulin depletion in human islets.

Animal Protocol

phosphate-buffered saline, pH 7.4; 0.01, 0.1, 1, 10, and 100 nmol/kg; i.p.

Male db/db mice C57BLKS/J-Leprdb/Leprdb

References

[1]. Core Evid . 2011:6:67-79.

[2]. J Pharmacol Exp Ther . 2003 Nov;307(2):490-6.

[3]. Regul Pept . 2010 Sep 24;164(2-3):58-64.

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

Physicochemical Properties

Molecular Formula

C215H347N61O65S

Molecular Weight

4858.49037999996

Exact Mass

4855.54

Elemental Analysis

C, 53.15; H, 7.20; N, 17.59; O, 21.40; S, 0.66

CAS #

320367-13-3

Related CAS #

Lixisenatide acetate; 1997361-87-1

Sequence

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2.

Appearance

Solid powder

InChi Key

XVVOERDUTLJJHN-UHFFFAOYSA-N

InChi Code

InChI=1S/C215H347N61O65S/c1-16-115(10)173(210(337)256-141(68-74-170(299)300)194(321)261-148(94-122-98-232-126-50-24-23-49-124(122)126)199(326)258-143(89-111(2)3)196(323)247-134(58-32-40-83-223)189(316)262-149(96-160(226)285)180(307)235-100-161(286)233-104-165(290)274-85-42-60-156(274)207(334)267-154(108-280)206(333)265-151(105-277)181(308)237-101-162(287)239-117(12)213(340)276-87-44-62-158(276)214(341)275-86-43-61-157(275)208(335)268-153(107-279)204(331)249-132(56-30-38-81-221)187(314)246-131(55-29-37-80-220)186(313)245-130(54-28-36-79-219)185(312)244-129(53-27-35-78-218)184(311)243-128(52-26-34-77-217)183(310)242-127(176(227)303)51-25-33-76-216)272-201(328)146(92-120-45-19-17-20-46-120)260-197(324)144(90-112(4)5)257-190(317)135(59-41-84-231-215(228)229)255-209(336)172(114(8)9)271-177(304)116(11)240-182(309)138(65-71-167(293)294)251-192(319)139(66-72-168(295)296)252-193(320)140(67-73-169(297)298)253-195(322)142(75-88-342-15)254-191(318)137(63-69-159(225)284)250-188(315)133(57-31-39-82-222)248-203(330)152(106-278)266-198(325)145(91-113(6)7)259-200(327)150(97-171(301)302)263-205(332)155(109-281)269-212(339)175(119(14)283)273-202(329)147(93-121-47-21-18-22-48-121)264-211(338)174(118(13)282)270-164(289)103-236-179(306)136(64-70-166(291)292)241-163(288)102-234-178(305)125(224)95-123-99-230-110-238-123/h17-24,45-50,98-99,110-119,125,127-158,172-175,232,277-283H,16,25-44,51-97,100-109,216-224H2,1-15H3,(H2,225,284)(H2,226,285)(H2,227,303)(H,230,238)(H,233,286)(H,234,305)(H,235,307)(H,236,306)(H,237,308)(H,239,287)(H,240,309)(H,241,288)(H,242,310)(H,243,311)(H,244,312)(H,245,313)(H,246,314)(H,247,323)(H,248,330)(H,249,331)(H,250,315)(H,251,319)(H,252,320)(H,253,322)(H,254,318)(H,255,336)(H,256,337)(H,257,317)(H,258,326)(H,259,327)(H,260,324)(H,261,321)(H,262,316)(H,263,332)(H,264,338)(H,265,333)(H,266,325)(H,267,334)(H,268,335)(H,269,339)(H,270,289)(H,271,304)(H,272,328)(H,273,329)(H,291,292)(H,293,294)(H,295,296)(H,297,298)(H,299,300)(H,301,302)(H4,228,229,231)

Chemical Name

5-[[2-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[6-amino-1-[[5-amino-1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[6-amino-1-[[4-amino-1-[[2-[[2-[2-[[1-[[1-[[2-[[1-[2-[2-[[1-[[6-amino-1-[[6-amino-1-[[6-amino-1-[[6-amino-1-[[6-amino-1-[(1,6-diamino-1-oxohexan-2-yl)amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoic acid

Synonyms

Lyxumia; Adlyxin; ZP10A peptide; ZP10 A peptide; ZP10-A peptide; AVE-0010; AVE0010; AVE 0010

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, avoid exposure to moisture.

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: N/A

Water: ~100 mg/mL (~20.6 mM)

Ethanol: N/A

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)

Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

Oral Formulations

Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.2058 mL	1.0291 mL	2.0583 mL
	5 mM	0.0412 mL	0.2058 mL	0.4117 mL
	10 mM	0.0206 mL	0.1029 mL	0.2058 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

Mass

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
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?

Enter 350.26 in the Molecular Weight (MW) box
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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

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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
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

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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Average weight of animals g

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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
NCT05804513	Recruiting	Drug: Placebo Drug: Lixisenatide 10 micrograms (50 micrograms/ml in 3 ml) Pen Injector	Healthy Type 1 Diabetes	University of Tartu	April 17, 2023	Phase 4
NCT02020629	Completed	Drug: Lixisenatide	Type 2 Diabetes	Lund University	December 2013	Phase 4
NCT02049034	Completed	Other: Lixisenatide Other: Placebo	Type 2 Diabetes	University of Surrey	January 2014	Phase 4
NCT03439943	Completed	Drug: Lixisenatide Drug: placebo	Parkinson Disease	University Hospital, Toulouse	June 13, 2018	Phase 2
NCT02276196	Completed	Drug: Lixisenatide Drug: Insulin glulisine	Diabetic Kidney Disease Diabetic Nephropathy	Amsterdam UMC, location VUmc	September 2014	Phase 4

Biological Data

Mean insulin secretion rate after an intravenous glucose challenge following injection of lixisenatide 20 μg or placebo.Core Evid.2011;6:67-79.
Least squares mean change in HbA1c after 13 weeks of treatment with lixisenatide once-daily or twice-daily according to dosage and regimen.20Core Evid.2011;6:67-79.
Least squares mean change in body weight after 13 weeks of treatment with lixisenatide once-daily or twice-daily according to dosage and regimen.Core Evid.2011;6:67-79.