Exendin 4 (4–39)
GTFTSDLSKQMEEEAVRLFIE-W-LKNGGPSSGAPPPS-amide
Description
Application Data
Description
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Amino acids 4-39 of exendin-4, a cleavage-resistant analogue of GLP-1 that stimulates insulin release.
Application Data
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Catalogue number crb1000423 Molecular Weight 3860.9 Sequence (one letter code) GTFTSDLSKQMEEEAVRLFIE-W-LKNGGPSSGAPPPS-amide
Sequence (three letter code) H-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
Purity >95% 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.
Manufactured in: United Kingdom This is a truncated exendin-4 peptide, the original peptide was 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.
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