Disitertide TFA
(Synonyms: P144 TFA) 目录号 : GC60782
Disitertide (P144)是转化生长因子β1（TGF-β1）受体I型的特异性抑制剂。
Sample solution is provided at 25 µL, 10mM.
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Disitertide (P144) is a specific inhibitor of transforming growth factor β1 (TGF-β1) receptor type I [1]. Disitertide binds to the TGF-β1 receptor, blocking the TGF-β1 signaling pathway and inhibiting extracellular matrix deposition and fibrotic responses, thereby slowing or reversing the progression of fibrosis [2-3]. Disitertide is primarily used to treat fibrotic diseases of various organs [4].
In LINC00941-overexpressing HCT-116 cells, Disitertide (10μM; 12h) treated cell showed increased mRNA and protein levels of ZO-1 and E-cadherin [5]. In LN229 cells, after Disitertide (100µg/mL; 10d) stimulation, SKI gene expression was significantly inhibited [6]. In MGC803 cells, Disitertide (20μM; 48h) blocks TGFβ1 signaling and effectively rescues the inhibitory effect of MFSD2A deficiency on CD8+ T cells [7].
In fibrosis rabbit mode, the macroscopic and microscopic morphology of muscles in the Disitertide (3.5mg/kg; iv; 72h) treated group was preserved, and extracellular matrix fibrosis was reduced [8].
References:
[1]. Neuzillet C, Tijeras-Raballand A, Cohen R, et al. Targeting the TGFβ pathway for cancer therapy[J]. Pharmacology & therapeutics, 2015, 147: 22-31.
[2]. Yang J, Zhuang Y, Liu J. Upregulation of microRNA‑590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor‑β1/phosphoinositide 3‑kinase/Akt signaling[J]. International Journal of Molecular Medicine, 2019, 43(5): 2212-2220.
[3]. He W, Liang B, Wang C, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer[J]. Oncogene, 2019, 38(23): 4637-4654.
[4]. Miwa S, Yokota M, Ueyama Y, et al. Discovery of selective transforming growth factor β type II receptor inhibitors as antifibrosis agents[J]. ACS Medicinal Chemistry Letters, 2021, 12(5): 745-751.
[5]. Wu N, Jiang M, Liu H, et al. LINC00941 promotes CRC metastasis through preventing SMAD4 protein degradation and activating the TGF-β/SMAD2/3 signaling pathway[J]. Cell Death & Differentiation, 2021, 28(1): 219-232.
[6]. Kubelt C, Hellmold D, Esser D, et al. Insights into gene regulation under temozolomide-promoted cellular dormancy and its connection to stemness in human glioblastoma[J]. Cells, 2023, 12(11): 1491.
[7]. Zhang B, Wang C M, Wu H X, et al. MFSD2A potentiates gastric cancer response to anti‐PD‐1 immunotherapy by reprogramming the tumor microenvironment to activate T cell response[J]. Cancer Communications, 2023, 43(10): 1097-1116.
[8]. Cruz-Morande S, Dotor J, San-Julian M. P144 a transforming growth factor beta inhibitor peptide, generates antifibrogenic effects in a radiotherapy induced fibrosis model[J]. Current Oncology, 2022, 29(4): 2650-2661.
Disitertide (P144)是转化生长因子β1（TGF-β1）受体I型的特异性抑制剂 [1]。Disitertide与TGF-β1受体结合，阻断TGF-β1信号通路，抑制细胞外基质沉积和纤维化反应，从而减缓或逆转纤维化的进展 [2-3]。Disitertide主要用于治疗各种器官的纤维化疾病 [4]。
在LINC00941过表达的HCT-116细胞中，Disitertide（10μM; 12h）处理的细胞中ZO-1和E-钙粘蛋白的mRNA和蛋白质水平升高 [5]。在LN229细胞中，经Disitertide（100µg/mL；10d）刺激后，SKI基因表达受到显著抑制 [6]。在MGC803细胞中，Disitertide（20μM；48h）可阻断TGFβ1信号传导，并有效挽救MFSD2A缺陷对CD8+T细胞的抑制作用 [7]。
在纤维化兔模型中，Disitertide（3.5mg/kg；iv；72h）治疗组肌肉的宏观和微观形态均得以保留，细胞外基质纤维化减轻 [8]。
| Cell experiment [1]: | |
Cell lines | LINC00941-overexpressing HCT-116 cells |
Preparation Method | Before TGF-β1 or Disitertide treatment, the cells were incubated with DMEM medium containing 10% FBS and 1% penicillin/streptomycin to achieve 80% cell fusion. Next, the cells were treated with TGF-β1 (0.2ng/mL) or Disitertide (10μM) for 12h. |
Reaction Conditions | 10μM; 12h |
Applications | Disitertide-treated LINC00941-overexpressing HCT-116 cells showed increased mRNA and protein levels of ZO-1 and E-cadherin. |
| Animal experiment [2]: | |
Animal models | Fibrosis rabbit model |
Preparation Method | Disitertide was stored at −80℃ before the manipulation peptide vial was tempered to room temperature and then weighed, resuspended in buffer diazonium salt of carbonic acid 0.1M pH 9.5, and sonicated until a homogeneous solution was obtained. Disitertide was IV in the marginal ear veins of the rabbits at doses 10mg per administration diluted in 10mL of buffer (approximately 3.5mg/kg). |
Dosage form | 3.5mg/kg; iv; 72h |
Applications | The macroscopic and microscopic morphology of muscles in the Disitertide treated group was preserved, and extracellular matrix fibrosis was reduced. |
References: | |
| Cas No. | SDF | ||
| 别名 | P144 TFA | ||
| 分子式 | C70H110N17O24S2F3 | 分子量 | 1694.84 |
| 溶解度 | 储存条件 | -20°C, protect from light | |
| 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 | 0.59 mL | 2.9501 mL | 5.9003 mL |
| 5 mM | 0.118 mL | 0.59 mL | 1.1801 mL |
| 10 mM | 0.059 mL | 0.295 mL | 0.59 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: >96.00%
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