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Submit ReviewExendin-3 (9-39) amide is a potent and selective GLP-1 receptor antagonist (Kd = 1.7 nM at cloned human GLP-1 receptors). Inhibits cAMP production and insulin release induced by GLP-1 (7-36), exendin-3 (IC50 = 20 nM) and exendin-4. Blocks the inhibitory effect of GLP-1 on food intake in rats.
分子量 | 3369.79 |
公式 | C149H234N40O47S |
序列 |
DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS (Modifications: Ser-31 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 133514-43-9 |
PubChem ID | 16198321 |
InChI Key | WSEVKKHALHSUMB-MVNVRWBSSA-N |
Smiles | [H]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。
Raufman et al (1991) Exendin-3, a novel peptide from the Heloderma horridum venom, interacts with vasoactive intestinal peptide receptors and a newly described receptor on dispersed acini from guinea pig pancreas. J.Biol.Chem. 266 2897 PMID: 1704369
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
Turton et al (1996) A role for glucagon-like peptide-1 in the central regulation of feeding. Nature 379 69 PMID: 8538742
If you know of a relevant reference for Exendin-3 (9-39) amide, please let us know.
关键词: Exendin-3 (9-39) amide, Exendin-3 (9-39) amide supplier, Potent, GLP-1, receptor, antagonists, Receptors, Glucagon-Like, Peptide, 1, 2081, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Exendin-3 (9-39) amide 的部分引用包括:
Gaitonde et al (2012) The role of the gut hormone GLP-1 in the metabolic improvements caused by ileal transposition. J Surg Res 178 33 PMID: 22929182
Maniscalco et al (2015) Negative Energy Balance Blocks Neural and Behavioral Responses to Acute Stress by " Silencing" Central Glucagon-Like Peptide 1 Signaling in Rats. Emerg Microbes Infect 35 10701 PMID: 26224855
Vallof et al (2019) Glucagon-like peptide-1 receptors within the nucleus of the solitary tract regulate alcohol-mediated behaviors in rodents. Neuropharmacology
Tuesta (2017) GLP-1 acts on habenular avoidance circuits to control nicotine intake. Nat Neurosci 20 708 PMID: 28368384
Bauer et al (2018) Lactobacillus gasseri in the Upper Small Intestine Impacts an ACSL3-Dependent Fatty Acid-Sensing Pathway Regulating Whole-Body Glucose Homeostasis. Cell Metab 27 572 PMID: 29514066
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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.