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Submit ReviewExendin-4 is a high affinity glucagon-like peptide 1 (GLP-1) receptor agonist (Kd = 136 pM); originally isolated from Heloderma suspectum venom. Exendin-4 potently induces cAMP formation without stimulating amylase release in pancreatic acini. Potentiates glucose-induced insulin secretion in isolated rat islets. Exendin-4 protects against glutamate-induced neurotoxicity, and in a mouse model of metabolic imblance it reduces neuroinflammation and enhances long-term-potentiation.
分子量 | 4186.61 |
公式 | C184H282N50O60S |
序列 |
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS (Modifications: Ser-39 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 141758-74-9 |
PubChem ID | 16157882 |
InChI Key | HTQBXNHDCUEHJF-XWLPCZSASA-N |
Smiles | [H]N[C@@H](CC1=CNC=N1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
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溶解性 | Soluble to 1 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Eng et al (1992) Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. J.Biol.Chem. 267 7402 PMID: 1313797
Goke et al (1993) Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of Ins-Secr.g β-cells. J.Biol.Chem. 268 19650 PMID: 8396143
Thorens et al (1993) Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor. Diabetes 42 1678 PMID: 8405712
Perry et al (2002) Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4. J.Pharmacol.Exp.Ther. 302 881 PMID: 12183643
Wang et al (2021) Exendin-4 improves long-term potentiation and neuronal dendritic growth in vivo and in vitro obesity condition. Sci.Rep. 11 8326 PMID: 33859286
If you know of a relevant reference for Exendin-4, please let us know.
关键词: Exendin-4, Exendin-4 supplier, Potent, GLP-1, receptor, agonists, Receptors, Glucagon-Like, Peptide, 1, AC2993, Ex4, exenatide, neuroprotective, neuroinflammation, neurotoxicity, LTP, Exenatide, AC, 2993, 1933, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Exendin-4 的部分引用包括:
Wang et al (2013) Glucagon-like peptide-1 protects against cardiac microvascular injury in diabetes via a cAMP/PKA/Rho-dependent mechanism. PLoS One 62 1697 PMID: 23364453
Suissa et al (2013) Gastrin: a distinct fate of neurogenin3 positive progenitor cells in the embryonic pancreas. ACS Chem Biol 8 e70397 PMID: 23940571
Vallof et al (2019) Glucagon-like peptide-1 receptors within the nucleus of the solitary tract regulate alcohol-mediated behaviors in rodents. Neuropharmacology 149 124 PMID: 30772374
Jazayeri (2017) Crystal structure of the GLP-1 receptor bound to a peptide agonist. Nature 546 254 PMID: 28562586
Lutter (2017) Novel and ultra-rare damaging variants in neuropeptide signaling are associated with disordered eating behaviors. PLoS One 12 e0181556 PMID: 28846695
Jesinkey et al (2019) Mitochondrial GTP Links Nutrient Sensing to β Cell Health, Mitochondrial Morphology, and Ins. Secretion Independent of OxPhos. Cell Rep 28 759 PMID: 31315053
Tuesta (2017) GLP-1 acts on habenular avoidance circuits to control nicotine intake. Nat Neurosci 20 708 PMID: 28368384
Pritchett and Hajnal (2012) Glucagon-like peptide-1 regulation of carbohydrate intake is differentially affected by obesogenic diets. Obesity (Silver Spring) 20 313 PMID: 22134200
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.