Exendin-4 [Lys(AF647)]
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-[K(AF647 DBCO)]-amide
Description
Application Data
Description
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Exendin-4 [Lys(AF647)] is a cleavage-resistant analogue of GLP-1 that stimulates insulin secretion; a C-terminal structural analog to Alexa Fluor® 647 is attached.
Application Data
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Catalogue number crb1101572 Molecular Weight 5454.4 Sequence (one letter code) HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-[K(AF647 DBCO)]-amide
Sequence (three letter code) H-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-Pro-Ser-[Lys(AF647 DBCO)]-NH2
Modifications Lys(AF647 DBCO) Purity >95% cas 141758-74-9 Storage -20°C References Kolterman, O. G., Kim, D. D., Shen L., Ruggles J. A., Nielsen L. L., Fineman M. S., Baron A. D. (2005) Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus. Am J Health Syst Pharm 62: 173–181. PMID: 15700891
Liao, S., Liang, Y., Zhang, Z., Li, J., Wang, J., Wang, X., Dou, G., Zhang, Z. and Liu, K. (2015). In Vitro Metabolic Stability of Exendin-4: Pharmacokinetics and Identification of Cleavage Products. PLOS ONE, 10(2), e0116805.
Luciani, P., Deledda, C., Benvenuti, S., Squecco, R., Cellai, I., Fibbi, B., Marone, I., Giuliani, C., Modi, G., Francini, F., Vannelli, G. and Peri, A. (2013). Exendin-4 Induces Cell Adhesion and Differentiation and Counteracts the Invasive Potential of Human Neuroblastoma Cells. PLoS ONE, 8(8), e71716. PMID: 23990978
Manufactured in: United Kingdom Exendin-4 is part of a group of peptide hormones, the exendins. These are members of the glucagon superfamily of peptides and are secreted from the Gila monster lizard (Heloderma suspectum) venom gland. Exendins stimulate insulin secretion in response to rising blood glucose levels and modulate gastric emptying to slow the entry of ingested sugars into the bloodstream. Exendin-4 increases insulin sensitivity and improves glucose tolerance in humans and animals with diabetes. Exendin-4 is currently used for treating type 2 diabetes mellitus in its synthetic form, Exenatide.
Exendin-4 shares 53% sequence homology, and specific activities, with glucagon-like-peptide-1 (GLP-1). Enteroendocrine L-cells produce GLP-1 upon nutrient ingestion, its central role relates to insulin secretion. Unlike GLP-1, exendin-4 is resistant to cleavage by plasma dipeptidyl peptidase IV (DPP-IV), resulting in a longer half-life and duration of action than GLP-1, as well as greater potency in vivo. Exendin-4 binds and activates the glucagon-like peptide-1 receptor (GLP-1R). In addition to its role in insulin sensitivity, exendin-4 also has a role in pancreas development and has anti-cancer properties.
This exendin-4 contains AF647, a structural analog to Alexa Fluor® 647, a widely used far-red fluorescent dye. Its excitation is ideally suited to 594nm or 633nm. This dye is suited for low abundance targets as it has high initial brightness and a high photostability allowing detection of low abundance peptides. If you desire an alternative dye, please contact us to request a custom synthesis.
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