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Submit Review[D-Ala2]-GIP (human) is a highly potent GIP receptor agonist (EC50 = 630 ± 119 pM). Displays equivalent cAMP stimulating properties and improved resistance to enzymatic degradation compared to native GIP (Cat. No. 2084) in cells expressing wild type GIP receptor. Improves glucose tolerance, insulin release and cognitive function in various animal models of obesity and diabetes. Displays neuroprotective effects in an MPTP model of PD.
分子量 | 4983.58 |
公式 | C226H338N60O66S |
序列 |
YAEGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ (Modifications: Ala-2 = D-Ala) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 444073-04-5 |
Smiles | [H]N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@H](C)C(=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)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=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。
Hinke et al (2002) Dipeptidyl peptidase IV-resistant [D-Ala2]glucose-dependent Insotropic polypeptide (GIP) improves glucose tolerance in normal and obese diabetic rats. Diabetes. 51 652 PMID: 11872663
Porter et al (2011) Prolonged GIP receptor activation improves cognitive function, hippocampal synaptic plasticity and glucose homeostasis in high-fat fed mice. Eur.J.Pharmacol. 650 688 PMID: 21050845
Verma et al (2017) Effect of D-Ala2GIP, a stable GIP receptor agonist on MPTP-induced neuronal impairments in mice. Eur.J.Pharmacol. 804 38 PMID: 28366809
If you know of a relevant reference for [D-Ala2]-GIP (human), please let us know.
关键词: [D-Ala2]-GIP (human), [D-Ala2]-GIP (human) supplier, gastric, inhibitory, polypeptide, receptor, enzymatic, resistance, resistant, degradation, GIPR, glucose, dependent, insulinotropic, peptide, agonists, agonism, highly, potent, GIP, Receptors, 6699, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 [D-Ala2]-GIP (human) 的部分引用包括:
Frank et al (2022) A brainstem circuit for nausea suppression. Cell Rep 39 110953 PMID: 35705049
Bin et al (2020) Chronic glucose-dependent insulinotropic polypeptide receptor (GIPR) agonism desensitizes adipocyte GIPR activity mimicking functional GIPR antagonism. Nat Commun 11 4981 PMID: 33020469
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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.