Disitertide diammonium (Synonyms: P144 diammonium) |
| Catalog No.GC68333 |
Disitertide diammonium is a specific inhibitor of transforming growth factor β1 (TGF-β1) receptor type I.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Disitertide diammonium 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.
| 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 | ||
| Synonyms | P144 diammonium | ||
| Formula | C68H115N19O22S2 | M.Wt | 1614.88 |
| Solubility | DMSO : 10 mg/mL (6.19 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 619.2 μL | 3.0962 mL | 6.1924 mL |
| 5 mM | 123.8 μL | 619.2 μL | 1.2385 mL |
| 10 mM | 61.9 μL | 309.6 μL | 619.2 μL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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