AT-1002 TFA
目录号 : GC34477
AT-1002 TFA 是一种六聚体合成肽，可降低跨上皮细胞电阻（TEER）。
Sample solution is provided at 25 µL, 10mM.
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AT-1002 TFA is a six-mer synthetic peptide that decreases transepithelial electrical resistance (TEER)[1]. AT-1002 TFA changes the structure of actin and ZO-1 proteins in epithelial cells, dissolving the tight junction[2]. AT-1002 TFA is widely used as the delivery enhancer for accelerating transdermal siRNA delivery in mouse models[3]. AT-1002 TFA can be used to prepare a novel protein coronal cationic liposome to improve the intestinal internalization of oral drugs and prolong the intestinal absorption time[4].
In vitro, AT-1002 TFA treatment at 7mM for 3h caused redistribution of ZO-1 and rearrangement of actin in Caco-2 BBE cells [5].
In vivo, AT-1002 TFA (300μg in 200μl of normal saline) combined with salmon calcitonin (sCT) (10μg in 200μl of normal saline) administered (intratracheal instillation) for one hour resulted in increased sCT absorption in rat lungs[6].
References:
[1] Li M, Oliver E, Kitchens K M, et al. Structure–activity relationship studies of permeability modulating peptide AT-1002[J]. Bioorganic & medicinal chemistry letters, 2008, 18(16): 4584-4586.
[2] Khaleghi S, Ju J M, Lamba A, et al. The potential utility of tight junction regulation in celiac disease: focus on larazotide acetate[J]. Therapeutic advances in gastroenterology, 2016, 9(1): 37-49.
[3] Uchida T, Kanazawa T, Takashima Y, et al. Development of an efficient transdermal delivery system of small interfering RNA using functional peptides, Tat and AT-1002[J]. Chemical and Pharmaceutical Bulletin, 2011, 59(2): 196-201.
[4] Ding R, Zhao Z, He J, et al. Preparation, drug distribution, and in vivo evaluation of the safety of protein corona liposomes for liraglutide delivery[J]. Nanomaterials, 2023, 13(3): 540.
[5] Gopalakrishnan S, Durai M, Kitchens K, et al. Larazotide acetate regulates epithelial tight junctions in vitro and in vivo[J]. Peptides, 2012, 35(1): 86-94.
[6] Gopalakrishnan S, Pandey N, Tamiz A P, et al. Mechanism of action of ZOT-derived peptide AT-1002, a tight junction regulator and absorption enhancer[J]. International journal of pharmaceutics, 2009, 365(1-2): 121-130.
AT-1002 TFA 是一种六聚体合成肽，可降低跨上皮细胞电阻（TEER）[1]。AT-1002 TFA能改变上皮细胞中肌动蛋白和ZO-1蛋白的结构，从而溶解紧密连接[2]。AT-1002 TFA被广泛用作递送增强剂，以加速小鼠模型中的透皮siRNA递送[3]。AT-1002 TFA可用于制备一种新型蛋白冠状阳离子脂质体，以改善口服药物的肠道内化并延长肠道吸收时间[4]。
在体外，用7mM的AT-1002 TFA处理Caco-2 BBE细胞3小时，会导致ZO-1重新分布和肌动蛋白重排[5]。
在体内，将AT-1002 TFA（300μg溶于200μl生理盐水）与鲑鱼降钙素（sCT）（10μg溶于200μl生理盐水）联合通过气管内滴注给药一小时，增加了大鼠肺部对sCT的吸收[6]。
| Cell experiment [1]: | |
Cell lines | Caco-2 BBE cells |
Preparation Method | Caco-2 BBE cells were cultured in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, penicillin (100units/ml), streptomycin (100μg/ml), and human transferrin (100μg/ml). Cells were seeded in 12-well plates at a density of 1×105 cells per well. Caco-2 BBE cells were treated apically with AT-1002 TFA (7mM) at 37°C for 3h. After treatment, the cells were digested off the filter membrane by trypsin. Digested cells were washed with PBS, fixed with PBS containing 4% paraformaldehyde for 15min at room temperature, permeabilized with PBS containing 0.5% Triton X-100 for 5min at room temperature, and blocked with PBS containing 2% goat serum for 30min at room temperature. Cells were incubated with Alexa Fluor555-phalloidin for 1h at room temperature, washed with PBS, and 10,000 cells in each sample were analyzed. |
Reaction Conditions | 7mM; 3h |
Applications | AT-1002 TFA treatment caused disassembly of stress fibers in Caco-2 BBE cells and actin rearrangement. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Sprague-Dawley rats were housed in a standard environment with access to water and feed ad libitum. The rats were intratracheal instilled with 10μg sCT (dissolved in 200μl of normal saline) containing 0 or 300μg AT-1002 TFA. Blood samples were collected before and 60min after administration for the determination of the concentration of sCT in rat plasma. |
Dosage form | 300μg in 200μl of normal saline for once; intratracheal instillation |
Applications | AT-1002 TFA treatment significantly enhanced the concentrations of sCT in rats. |
References: | |
| Cas No. | SDF | ||
| Canonical SMILES | N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CS)C(N[C@@H]([C@H](CC)C)C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O | ||
| 分子式 | C34H54F3N9O9S | 分子量 | 821.91 |
| 溶解度 | DMSO : 33.33 mg/mL (40.55 mM; Need ultrasonic); H2O : 1 mg/mL (1.22 mM; Need ultrasonic) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2167 mL | 6.0834 mL | 12.1668 mL |
| 5 mM | 243.3 μL | 1.2167 mL | 2.4334 mL |
| 10 mM | 121.7 μL | 608.3 μL | 1.2167 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet