[Cys]-Exendin 4 [C]-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-amide
Description
Application Data
Description
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Exendin-4 is a cleavage resistant analogue of GLP-1 that stimulates insulin secretion; contains an N-terminal cysteine for conjugation reactions.
Application Data
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Catalogue number crb1000606 Molecular Weight 4287 Sequence (one letter code) [C]-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-amide Sequence (three letter code) [Cys]-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-NH2 Molecular Weight 4287 Purity >95% Storage -20°C References Kolterman et al., (2005). Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus. Am. J. Health Syst. Pharm., 62: 173. PMID: 15700891.
Liao et al., (2015). In Vitro Metabolic Stability of Exendin-4: Pharmacokinetics and Identification of Cleavage Products. PLOS ONE, 10(2): e0116805. PMID: 25723538.
Originally identified in Gila monster lizard (Heloderma suspectum), Exendin-4 is an incretin mimetic, an analog of glucagon-like-peptide-1 (GLP-1), it stimulates insulin secretion and modulates gastric emptying to slow the entry of ingested sugars into the bloodstream. Exendin-4 is resistant to cleavage by plasma DPP-IV unlike GLP-1. This gives it a longer half-life and duration of action than GLP-1, as well as greater potency in vivo. Exendin-4 increases insulin sensitivity and improves glucose tolerance and is currently used for the treatment of Type 2 diabetes mellitus in its synthetic form Exenatide.
Exendin-4 also promotes the production and proliferation of β-cells leading to regeneration of the pancreas. It is a ligand to the exendin receptor and increases pancreatic acinar cell cAMP levels. However, the GLP-1 analog was found to have a toxic effect by inducing hypotension due to relaxation of the cardiac smooth muscle.
This exendin-4 peptide is provided with an N-terminal cysteine residue for conjugation reactions.