Disitertide (P144) |
Catalog No.GC34060
One-Click Copy Product Info
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Disitertide (P144) es un inhibidor específico del receptor del factor de crecimiento transformador β1 (TGF-β1) tipo I
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 272105-42-7
Sample solution is provided at 25 µL, 10mM.
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Disitertide (P144) es un inhibidor específico del receptor del factor de crecimiento transformador β1 (TGF-β1) tipo I [1]. Disitertide se une al receptor TGF-β1, bloqueando la vía de señalización TGF-β1 e inhibiendo la deposición de la matriz extracelular y las respuestas fibróticas, ralentizando o revirtiendo así la progresión de la fibrosis[2-3]. Disitertide se utiliza principalmente para tratar enfermeddes fibróticas de varios órganos [4].
En las células HCT-116 que sobreexpresan LINC00941, Disitertide (10μM; 12h) mostró un aumento de los niveles de mRNA y proteínas de ZO-1 y E-cadherin [5]. En las células LN229, después de la estimulación de Disitertide (100µg/mL; 10d) , la expresión del gen SKI se inhibió significativamente[6]. En las células MGC803, Disitertide (20μM; 48h) bloquea la señalización de TGFβ1 y rescata eficamente el efecto inhibidor de la deficiencia de MFSD2A en las células CD8+ T [7].
En el modelo de conejo con fibrosis, se conservó la morfología macxrocópica y el grupo tratado con Disitertide (3.5mg/kg; iv; 72h) y se redujo la fibrosis de la matriz extracelular [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.
| Experimentos celulares [1]: | |
Líneas celulares | LINC00941-sobreexpresión de células HCT-116 |
Método de preparación | Antes del tratamiento con TGF-β1 o Disitertide, las células se incubaron con medio DMEM que contenía un 10% de FBS y un 1% de penicilina/estreptomicina para lograr una fusión celular del 80%. A continuación, las células fueron tratadas con TGF-β1 (0,2 ng/mL) o Disitertide (10μM) durante 12 horas. |
Condiciones de reacción | 10 μM; 12h |
Áreas de aplicación | Las células HCT-116 sobreexpresadas con LINC00941 tratadas con Disitertide mostraron un aumento de los niveles de ARNm y proteína de ZO-1 y E-cadherina. |
| Experimentos con animales [2]: | |
Modelos animales | Modelo de conejo de fibrosis |
Método de preparación | Disitertide se almacenó a -80℃ antes de que el vial de péptido de manipulación se templara a temperatura ambiente y luego se pesara, se resuspende en sal de diazonio de tampón de ácido carbónico 0,1 m pH 9,5, y se sonica hasta que se obtuvo una solución homogénea. Disitertide fue IV en las venas marginales del oído de los conejos a dosis de 10 mg por administración diluidas en 10 ml de tampón (aproximadamente 3,5 mg/kg). |
Forma de dosificación | 3,5mg/kg; iv; 72h |
Áreas de aplicación | Se conservó la morfología macroscópica y microscópica de los músculos en el grupo tratado con Disitertide, y se redujo la fibrosis de la matriz extracelular. |
References: | |
| Cas No. | 272105-42-7 | SDF | |
| Canonical SMILES | Thr-Ser-Leu-Asp-Ala-Ser-Ile-Ile-Trp-Ala-Met-Met-Gln-Asn | ||
| Formula | C68H109N17O22S2 | M.Wt | 1580.82 |
| Solubility | DMSO : ≥ 200 mg/mL (126.52 mM);Water : < 0.1 mg/mL (insoluble) | 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. |
||
| 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 | 632.6 μL | 3.1629 mL | 6.3258 mL |
| 5 mM | 126.5 μL | 632.6 μL | 1.2652 mL |
| 10 mM | 63.3 μL | 316.3 μL | 632.6 μL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)