GlpBio

Larazotide acetate

目录号: GC33822纯度: >98.50%同义词: 醋酸拉瑞唑来
Larazotide acetate（以前称为 AT-001）是一种高度极性的八肽，来源于霍乱弧菌分泌的原核闭合带蛋白。
Larazotide acetate
Cas No.: 881851-50-9
规格价格库存数量操作
1mg¥630.00现货
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5mg¥990.00现货
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10mg¥1,620.00现货
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25mg¥3,240.00现货
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10mm*1mlinwater¥1,400.00现货
1
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产品描述 Description

Larazotide acetate (formerly AT-001) is a highly polar octapeptide, derived from a prokaryotic zonula occludens protein secreted by Vibrio cholera[6].

In vitro studies have shown larazotide acetate can prevent the opening of tight junctions, induced by cytokines, bacterial agents and gluten fragments[7,8]. In Lucifer yellow (LY) permeability assays, AT-1002 induces TJ barrier dysfunction in human-derived Caco-2 cells[2], AT-1002 caused a substantial increase in LY passage, which was inhibited by larazotide acetate in a dose-dependent manner. Larazotide acetate at 15 and 12.5 mM significantly inhibited the AT-1002-induced increase in LY passage by 71 and 38%, respectively[1]. Larazotide acetate inhibits gliadin-induced cytoskeletal reorganization in IEC-6 cells[3].

In vivo in gliadin-sensitized HLA-HCD4/DQ8 double transgenic mice, Gliolidin-induced barrier function and macrophage recruitment were altered, larazotide acetate inhibited gliadin-induced macrophage accumulation in the intestine and preserved normal TJ structure[1].

larazotide acetate inhibited transport of gliadin peptides even at 0.1 mM. In animal experiments using BB Wor rats [4] and IL-10 / mice [5], the effective in vivo dose of larazotide acetate is on the order of 0.2-100 μM. Lupus-derived RG strains induced high levels of intestinal permeability that was significantly greater in female than male mice, Strikingly, gut permeability was completely reversed by oral treatment with larazotide acetate[9].

References:
[1]: Gopalakrishnan S, Durai M, et,al. Larazotide acetate regulates epithelial tight junctions in vitro and in vivo. Peptides. 2012 May;35(1):86-94. doi: 10.1016/j.peptides.2012.02.015. Epub 2012 Feb 27. PMID: 22401908.
[2]: Gopalakrishnan S, Pandey N, et,al. Mechanism of action of ZOT-derived peptide AT-1002, a tight junction regulator and absorption enhancer. Int J Pharm. 2009 Jan 5;365(1-2):121-30. doi: 10.1016/j.ijpharm.2008.08.047. Epub 2008 Sep 11. PMID: 18832018.
[3]: Clemente MG, De Virgiliis S, et,al. Early effects of gliadin on enterocyte intracellular signalling involved in intestinal barrier function. Gut. 2003 Feb;52(2):218-23. doi: 10.1136/gut.52.2.218. PMID: 12524403; PMCID: PMC1774976.
[4]: Watts T, Berti I, et,al. Role of the intestinal tight junction modulator zonulin in the pathogenesis of type I diabetes in BB diabetic-prone rats. Proc Natl Acad Sci U S A. 2005 Feb 22;102(8):2916-21. doi: 10.1073/pnas.0500178102. Epub 2005 Feb 14. PMID: 15710870; PMCID: PMC549484.
[5]: Arrieta MC, Bistritz L, et,al. Alterations in intestinal permeability. Gut. 2006 Oct;55(10):1512-20. doi: 10.1136/gut.2005.085373. PMID: 16966705; PMCID: PMC1856434.
[6]: Wang W, Uzzau S, et,al. Human zonulin, a potential modulator of intestinal tight junctions. J Cell Sci. 2000 Dec;113 Pt 24:4435-40. doi: 10.1242/jcs.113.24.4435. PMID: 11082037.
[7]: Gopalakrishnan S, Tripathi A, et,al. Larazotide acetate promotes tight junction assembly in epithelial cells. Peptides. 2012 May;35(1):95-101. doi: 10.1016/j.peptides.2012.02.016. Epub 2012 Feb 28. PMID: 22401910.
[8]: Sturgeon C, Fasano A. Zonulin, a regulator of epithelial and endothelial barrier functions, and its involvement in chronic inflammatory diseases. Tissue Barriers. 2016 Oct 21;4(4):e1251384. doi: 10.1080/21688370.2016.1251384. PMID: 28123927; PMCID: PMC5214347.
[9]: Silverman GJ, Deng J,et,al. Sex-dependent Lupus Blautia (Ruminococcus) gnavus strain induction of zonulin-mediated intestinal permeability and autoimmunity. Front Immunol. 2022 Aug 11;13:897971. doi: 10.3389/fimmu.2022.897971. PMID: 36032126; PMCID: PMC9405438.

Larazotide acetate（以前称为 AT-001）是一种高度极性的八肽，来源于霍乱弧菌[6]分泌的原核闭合带蛋白。

体外研究表明，醋酸拉拉扎肽可以防止由细胞因子、细菌制剂和麸质片段诱导的紧密连接打开[7,8]。在路西法黄 (LY) 通透性测定中，AT-1002 诱导人源 Caco-2 细胞的 TJ 屏障功能障碍[2]，AT-1002 导致 LY 传代显着增加，这被抑制Larazotide acetate 呈剂量依赖性。 15 和 12.5 mM 的醋酸拉拉扎肽分别显着抑制 AT-1002 诱导的 LY 传代增加 71% 和 38%[1]。 Larazotide acetate抑制麦醇溶蛋白诱导的IEC-6细胞骨架重组[3]。

在麦醇溶蛋白致敏的 HLA-HCD4/DQ8 双转基因小鼠体内，麦醇溶蛋白诱导的屏障功能和巨噬细胞募集发生改变，醋酸拉拉扎肽抑制麦醇溶蛋白诱导的巨噬细胞在肠道中的积累并保持正常的 TJ 结构[1 ].

larazotide acetate 甚至在 0.1 mM 时也能抑制麦醇溶蛋白肽的转运。在使用BB Wor大鼠[4]和IL-10/小鼠[5]的动物实验中，醋酸拉拉扎肽的体内有效剂量为0.2-100微米。狼疮衍生的 RG 菌株诱导高水平的肠道通透性，雌性小鼠明显高于雄性小鼠。令人惊讶的是，口服醋酸拉拉扎肽[9]可完全逆转肠道通透性。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Caco-2 and IEC6 cells

Preparation Method

Treatment solutions containing LY with or without AT-1002 and different concentrations of larazotide acetate in HBSS were added to the apical compartment of each monolayer and incubated at 37 °C, 50 rpm for 180 min.

Reaction Conditions

0-15mM larazotide acetate at 37 °C for 60 min or 180 min,

Applications

In Lucifer yellow (LY) permeability assays, AT-1002 caused a substantial increase in LY passage, which was inhibited by larazotide acetate in a dose-dependent manner. Larazotide acetate at 15 and 12.5 mM significantly inhibited the AT-1002-induced increase in LY passage by 71 and 38%, respectively.
Animal experiment [1]:

Animal models

HLA-HCD4/DQ8 mice

Preparation Method

Mice were gavaged with gliadin (2 mg/mouse), +/ treatment, 2 /week for 7 weeks. Group 1 received larazotide acetate (250 μg/mouse) and gliadin.

Dosage form

250 μg larazotide acetate /mouse, twice a week for 7 weeks

Applications

In vivo in gliadin-sensitized HLA-HCD4/DQ8 double transgenic mice, larazotide acetate inhibited gliadin-induced macrophage accumulation in the intestine and preserved normal TJ structure.

References:

[1]. Gopalakrishnan S, Durai M, et,al. Larazotide acetate regulates epithelial tight junctions in vitro and in vivo. Peptides. 2012 May;35(1):86-94. doi: 10.1016/j.peptides.2012.02.015. Epub 2012 Feb 27. PMID: 22401908.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
881851-50-9
同义词
醋酸拉瑞唑来
SMILES
O=C([C@H](C(C)C)NC([C@H](CC(C)C)NC([C@H](C(C)C)NC(CNC(CN)=O)=O)=O)=O)N[C@@H](CCC(N)=O)C(N1[C@@H](CCC1)C(NCC(O)=O)=O)=O.CC(O)=O
分子式
C34H59N9O12
分子量
785.89 g/mol
溶解性
Water : 16.67 mg/mL (21.21 mM);DMSO : 3.2 mg/mL (4.07 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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