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Submit ReviewAC 187 is an orally active, potent amylin receptor antagonist (IC50 = 0.48 nM) that displays 38-fold and 400-fold selectivity over calcitonin and CGRP receptors respectively. Blocks amyloid β-induced neurotoxicity by attenuating the activation of initiator and effector caspases in vitro. Increases glucagon secretion, accelerates gastric emptying, alters plasma glucose levels and increases food intake in vivo.
分子量 | 2890.25 |
公式 | C127H205N37O40 |
序列 |
VLGKLSQELHKLQTYPRTNTGSNTY (Modifications: Val-1 = N-terminal Ac, Tyr-25 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 151804-77-2 |
PubChem ID | 16133792 |
InChI Key | ZLFXHYNEZYAYPG-AABHONRUSA-N |
Smiles | CC(C)C[C@H](NC(=O)[C@@H](NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)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。
Tocris products are intended for laboratory research use only, unless stated otherwise.
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。
Jhamandas and MacTavish (2004) Antagonist of the amylin receptor blocks β-amyloid toxicity in rat cholinergic basal forebrain neurons. J.Neurosci. 24 5579 PMID: 15201330
Gedulin et al (2006) Role of endogenous amylin in glucagon secretion and gastric emptying in rats demonstrated with the selective antagonist, AC187. Regul.Pept. 137 121 PMID: 16914214
Reidelberger et al (2004) Amylin receptor blockade stimulates food intake in rats. Am.J.Physiol.Inter.Comp.Physiol. 287 R568
If you know of a relevant reference for AC 187, please let us know.
关键词: AC 187, AC 187 supplier, Potent, selective, amylin, receptors, antagonists, AC187, Calcitonin, and, Related, Receptors, 3419, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AC 187 的部分引用包括:
Liberini et al (2016) The satiating hormone amylin enhances neurogenesis in the area postrema of adult rats. Mol Metab 5 834 PMID: 27688997
Baisley et al (2014) Antipsychotic-like actions of the satiety peptide, amylin, in ventral striatal regions marked by overlapping calcitonin receptor and RAMP-1 gene expression. J Neurosci 34 4318 PMID: 24647952
Nuñez-Diaz et al (2023) Contraction of human brain vascular pericytes in response to islet amyloid polypeptide is reversed by pramlintide. Mol Brain 16 25 PMID: 36793056
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.