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Merck
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Key Documents

SML2836

Sigma-Aldrich

Lixisenatide

≥95% (HPLC)

Sinónimos:

(Des-Pro38)-Exendin-4-(Lys)6 amide, AVE0010, HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2, 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, ZP10, ZP10A

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About This Item

Fórmula empírica (notación de Hill):
C215H347N61O65S
Número de CAS:
Peso molecular:
4858.49
UNSPSC Code:
51111800
NACRES:
NA.77

Quality Level

assay

≥95% (HPLC)

form

lyophilized powder

color

white to beige

storage temp.

−20°C

Biochem/physiol Actions

Lixisenatide (AVE0010, ZP10A) is a C-terminal amidated synthetic glucagon-like peptide-1 receptor (GLP-1R) agonist peptide whose sequence corresponds to Pro38 deleted exendin-4 with a C-terminal extension by six Lys residues. Lixisenatide exhibits 4-times higher human GLP-1R affinity than GLP-1(7-36) amide and dispalys in vivo therapeutic efficacy in murine and rat models of type 2 diabetes, as well as rat models of dox-induced renal fibrosis, global cerebral I/R injury, abdominal aortic aneurysm (AAA) and Aβ25-35 toxicity.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Preclinical pharmacology of the new GLP-1 receptor agonist AVE0010.
U Werner
Annales d'endocrinologie, 69(2), 164-165 (2008-04-18)
Qini Zhao et al.
Artificial cells, nanomedicine, and biotechnology, 47(1), 2325-2332 (2019-06-09)
Increased free fatty acids (FFA) are one of the risk factors for type 2 diabetes. FFA also contribute to endothelial dysfunction in both the prediabetes and diabetes conditions. Therefore, FFA are an important link between diabetes and endothelial dysfunction. In
Ángela Vinué et al.
Diabetologia, 60(9), 1801-1812 (2017-06-14)
Recent clinical studies indicate that glucagon-like peptide-1 (GLP-1) analogues prevent acute cardiovascular events in type 2 diabetes mellitus but their mechanisms remain unknown. In the present study, the impact of GLP-1 analogues and their potential underlying molecular mechanisms in insulin
Julie Charpentier et al.
American journal of physiology. Gastrointestinal and liver physiology, 315(5), G671-G684 (2018-08-03)
Endogenous glucagon-like peptide-1 (GLP-1) regulates glucose-induced insulin secretion through both direct β-cell-dependent and indirect gut-brain axis-dependent pathways. However, little is known about the mode of action of the GLP-1 receptor agonist lixisenatide. We studied the effects of lixisenatide (intraperitoneal injection)
Christian Thorkildsen et al.
The Journal of pharmacology and experimental therapeutics, 307(2), 490-496 (2003-09-17)
We characterized the novel, rationally designed peptide glucagon-like peptide 1 (GLP-1) receptor agonist H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSK KKKKK-NH2 (ZP10A). Receptor binding studies demonstrated that the affinity of ZP10A for the human GLP-1 receptor was 4-fold greater than the affinity of GLP-1 (7-36) amide.

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