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GLP-2 analogue 10

功能和特点
有货

库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
rp174140-500μg
500μg 期货 Stock Image
rp174140-1mg
1mg 期货 Stock Image
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GLP-2 receptor Agonist

基本描述

产品名称 GLP-2 analogue 10

产品规格参数

CAS编号和信息 rp174140

关联配体

Ligand ID 9896
名称 GLP-2 analogue 10
类别 Peptide
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 GLP-2 analogue 10 exhibits more effective anti-inflammatory effects in mouse models of DSS-induced colitis than . The half-life of GLP-2 analogue 10 is 4.7 hours after i.v. administration, in contrast to teduglutide's half-life of 25 minutes.
评价 This GLP-2 analogue (peptide 10 in ) was designed to increase the peptide's metabolic stability (and in vivo pharmacokinetic profile) beyond that of the clinically approved DPP4 resistant GLP-2 analogue , with the aim of providing sustained therapeutic effects. GLP-2 analogue 10 achieves increased half-life by the incorporation of a covalent Cys-mediated side-chain cross-link (or staple) that stabilises the α-helical conformation of the peptide. The terminal PSSGAPPPS sequence of 10 is the C-terminal extension of which improves the peptide's solubility.
The intestinotrophic effects of GLP-2 (e.g. promotion of intestinal growth, reduced epithelial cell apoptosis and inflammation) has led to the development of GLP-2 analogues for the treatment of GI disorders such as short bowel syndrome, inflammatory bowel diseases and potentially other intestinal insufficiency diseases.
单字母多肽序列 HGDGSFSDEMCTILDNLCARDFINWLIQTKITDPSSGAPPPS-NH2
三字母多肽序列
翻译后修饰
化学修饰 Cys residues 11 and 18 are covalently linked by the lipidated cross-linker L3 which contains a cysteine-reactive bis-bromoacetamide moiety .

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参考文献

1. Blonski W, Buchner AM, Aberra F, Lichtenstein G.  (2013)  Teduglutide in Crohn's disease..  Expert Opin Biol Ther,  13  (8):  (1207-14).  [PMID:23834252]
2. Kochar B, Long MD, Shelton E, Young L, Farraye FA, Yajnik V, Herfarth H.  (2017)  Safety and Efficacy of Teduglutide (Gattex) in Patients With Crohn's Disease and Need for Parenteral Support Due to Short Bowel Syndrome-associated Intestinal Failure..  J Clin Gastroenterol,  51  (6):  (508-511).  [PMID:27433811]
3. Yang PY, Zou H, Lee C, Muppidi A, Chao E, Fu Q, Luo X, Wang D, Schultz PG, Shen W.  (2018)  Stapled, Long-Acting Glucagon-like Peptide 2 Analog with Efficacy in Dextran Sodium Sulfate Induced Mouse Colitis Models..  J Med Chem,  61  (7):  (3218-3223).  [PMID:29528634]

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