MedChemExpress - Model Lixisenatide - 320367-13-3

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].

Lixisenatide

MCE China：Lixisenatide

Brand：MedChemExpress (MCE)

Cat. No.HY-P0119

CAS：320367-13-3

Purity：99.86%

Storage：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)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

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].

IC50 & Target：MEK1 MEK2 MMP13 MMP-1 MMP-3

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

References：

[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]

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