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> Lixisenatide [320367-13-3]

Lixisenatide [320367-13-3]

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Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe−/− Irs2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation.

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Synthèse de peptides personnalisée

Lixisenatide Chemical Structure

Lixisenatide Chemical Structure

CAS No. : 320367-13-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Lixisenatide:

  • Lixisenatide acetate In-stock

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Description

Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe−/− Irs2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation[2][3][5].

IC50 & Target

MEK1

 

MEK2

 

MMP13

 

MMP-1

 

MMP-3

 

In Vitro

Lixisenatide (100 μM, 24 h) inhibits the Aβ25-35-induced cytotoxicity on cultured hippocampal cells. [1].
Lixisenatide (100 μM, 24 h) relieves the Aβ25-35-induced suppression of the Akt-MEK1/2 signaling pathway on cultured hippocampal cells [1].
Lixisenatide (10-20 μM, 48 h) ameliorates IL-1β-induced oxidative stress, mitochondrial dysfunction, and apoptosis in fibroblast-like synoviocytes (FLSs) [3].
Lixisenatide (10-20 μM, 48 h) reduces IL-1β-induced expression of MMPs and inhibits activation of proinflammatory pathways by IL-1β in FLSs[3].
Lixisenatide (10-20 μM, 6 h) reduced oxygen-glucose deprivation/reperfusion (OGD/R)-induced generation of ROS in HUVECs[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lixisenatide Related Antibodies

Cell Viability Assay[1]

Cell Line: Hippocampal cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Reversed Aβ25-35-triggered cytotoxicity on hippocampal cell cultures.

Western Blot Analysis[3]

Cell Line: FLSs
Concentration: 10 μM, 20 μM
Incubation Time: 48 h
Result: Significantly reduced expression of MMP-1, MMP-3, and MMP-13 at both the mRNA and protein levels in a dose-dependent manner.
In Vivo

Lixisenatide (10 μg/kg, Subcutaneous injection, once a day for a month) diminishes the atherosclerosis burden and produces more stable plaques [2].
Lixisenatide (10 μg/kg, Subcutaneous injection, once a day for a month) decreases systemic inflammation in atherogenic-diet-fed Apoe−/− Irs2+/− mice[2].
Lixisenatide (1 nmol/kg, Intraperitoneal injection, once a day for 14 days) afford renoprotective effects on experimental early diabetic nephropathy in a low dose[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Apoe−/− Irs2+/− mice [2]
Dosage: 10 μg/kg
Administration: Subcutaneous injection (s.c.)
Result: Exhibited smaller atheromas in the aortic arch region.
Reduced the lesion size in cross-sections of hearts.
Animal Model: Diabetic rats [4]
Dosage: 1 nmol/kg
Administration: Intraperitoneal injection (i.p.)
Result: Showed a significant amelioration on the elevated renal parameters.
Showed significant mitigation in renal MDA and total NOx− (by 50.3 and 79.9%, respectively) and 43.9% elevation in renal total antioxidant capacity.
Averted the observed increments in iNOS and COX-2 expressions in the renal tissues of the diabetic group.
Decreased the level of TGF-β protein expression.
Essai clinique
Masse moléculaire

4858.49

Formule

C215H347N61O65S
CAS No.

320367-13-3
Appearance

Solid

Color

White to pink

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
Sequence Shortening

HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

H2O : 100 mg/mL (20.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureté et documentation
Références

  • [1]. Cai H Y, et al. Lixisenatide attenuates the detrimental effects of amyloid β protein on spatial working memory and hippocampal neurons in rats [J]. Behavioural brain research, 2017, 318: 28-35.  [Content Brief]

    [2]. Vinué Á, et al. The GLP-1 analogue lixisenatide decreases atherosclerosis in insulin-resistant mice by modulating macrophage phenotype [J]. Diabetologia, 2017, 60: 1801-1812.  [Content Brief]

    [3]. Du X, et al. The protective effects of lixisenatide against inflammatory response in human rheumatoid arthritis fibroblast-like synoviocytes [J]. International immunopharmacology, 2019, 75: 105732.  [Content Brief]

    [4]. Abdel-Latif R G, et al. Low-dose lixisenatide protects against early-onset nephropathy induced in diabetic rats [J]. Life Sciences, 2020, 263: 118592.  [Content Brief]

    [5]. Xiao M, et al. The protective effects of GLP-1 receptor agonist lixisenatide on oxygen-glucose deprivation/reperfusion (OGD/R)-induced deregulation of endothelial tube formation [J]. RSC advances, 2020, 10(17): 10245-10253.  [Content Brief]

    [6]. Ahrén B et al. Postprandial Glucagon Reductions Correlate to Reductions in Postprandial Glucose and Glycated Hemoglobin with Lixisenatide Treatment in Type 2 Diabetes Mellitus: A Post Hoc Analysis. Diabetes Ther. 2016 Jun 18  [Content Brief]

    [7]. Ulrich Werner, et al. Pharmacological profile of lixisenatide: A new GLP-1 receptor agonist for the treatment of type 2 diabetes. Regul Pept. 2010 Sep 24;164(2-3):58-64.  [Content Brief]

    [8]. Lorenz M, et al. Effects of lixisenatide once daily on gastric emptying in type 2 diabetes--relationship to postprandial glycemia. Regul Pept. 2013 Aug 10;185:1-8.  [Content Brief]

    [9]. Mikkel Christensen, et al. Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus. IDrugs. 2009 Aug;12(8):503-13.  [Content Brief]

    [10]. D Tews, et al. Enhanced protection against cytokine- and fatty acid-induced apoptosis in pancreatic beta cells by combined treatment with glucagon-like peptide-1 receptor agonists and insulin analogues. Horm Metab Res. 2008 Mar;40(3):172-80.  [Content Brief]

  • [1]. Cai H Y, et al. Lixisenatide attenuates the detrimental effects of amyloid β protein on spatial working memory and hippocampal neurons in rats [J]. Behavioural brain research, 2017, 318: 28-35.

    [2]. Vinué Á, et al. The GLP-1 analogue lixisenatide decreases atherosclerosis in insulin-resistant mice by modulating macrophage phenotype [J]. Diabetologia, 2017, 60: 1801-1812.

    [3]. Du X, et al. The protective effects of lixisenatide against inflammatory response in human rheumatoid arthritis fibroblast-like synoviocytes [J]. International immunopharmacology, 2019, 75: 105732.

    [4]. Abdel-Latif R G, et al. Low-dose lixisenatide protects against early-onset nephropathy induced in diabetic rats [J]. Life Sciences, 2020, 263: 118592.

    [5]. Xiao M, et al. The protective effects of GLP-1 receptor agonist lixisenatide on oxygen-glucose deprivation/reperfusion (OGD/R)-induced deregulation of endothelial tube formation [J]. RSC advances, 2020, 10(17): 10245-10253.

    [6]. Ahrén B et al. Postprandial Glucagon Reductions Correlate to Reductions in Postprandial Glucose and Glycated Hemoglobin with Lixisenatide Treatment in Type 2 Diabetes Mellitus: A Post Hoc Analysis. Diabetes Ther. 2016 Jun 18

    [7]. Ulrich Werner, et al. Pharmacological profile of lixisenatide: A new GLP-1 receptor agonist for the treatment of type 2 diabetes. Regul Pept. 2010 Sep 24;164(2-3):58-64.

    [8]. Lorenz M, et al. Effects of lixisenatide once daily on gastric emptying in type 2 diabetes--relationship to postprandial glycemia. Regul Pept. 2013 Aug 10;185:1-8.

    [9]. Mikkel Christensen, et al. Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus. IDrugs. 2009 Aug;12(8):503-13.

    [10]. D Tews, et al. Enhanced protection against cytokine- and fatty acid-induced apoptosis in pancreatic beta cells by combined treatment with glucagon-like peptide-1 receptor agonists and insulin analogues. Horm Metab Res. 2008 Mar;40(3):172-80.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.2058 mL 1.0291 mL 2.0583 mL 5.1456 mL
5 mM 0.0412 mL 0.2058 mL 0.4117 mL 1.0291 mL
10 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.5146 mL
15 mM 0.0137 mL 0.0686 mL 0.1372 mL 0.3430 mL
20 mM 0.0103 mL 0.0515 mL 0.1029 mL 0.2573 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Lixisenatide Related Classifications

  • Neurological Disease Metabolic Disease Inflammation/Immunology
  • GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR Metabolic Enzyme/Protease
  • GCGR MEK Akt MMP JNK
Help & FAQs

Keywords:

Lixisenatide320367-13-3GCGRMEKAktMMPJNKGlucagon ReceptorMitogen-activated protein kinase kinaseMAPKKMAP2KPKBProtein kinase BMatrix metalloproteinasesc-Jun N-terminal kinaseFibroblast-like synoviocytes (FLSs)Hippocampal cellsHuman umbilical vascular endothelial cells (HUVECs)DiabeticInhibitorinhibitorinhibit

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