| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
TGF-β1, P13K[1][2].
|
|---|---|
| ln Vitro |
In MC3T3-E1 cells, disitertide (P144, 100 μg/mL) TFA increases the production of Bax protein while suppressing PI3K and p-Akt [2]. TFA, an inhibitor of TGFβ1, suppresses the expression of MACC1-AS1 in GC cells, suggesting that a possible tactic to prevent MSC-induced stemness and chemotherapy resistance would be to target the TGFβ signaling pathway [3]. Disitertide (10 μg/mL to 200 μg/mL) TFA influences the growth, triggers apoptosis, and causes anoikis in GBM cell lines A172 and U-87 MG [5].
|
| ln Vivo |
After two weeks of therapy in a nude mouse "in vivo" model, dissolvertide (P144, Topical administration, 300 μg/mL) TFA improves the morphological aspects of hypertrophic scars and accelerates scar maturation [4].
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: Mouse embryo osteoblast precursor MC3T3-E1 cells. Tested Concentrations: 100 μg/mL. Incubation Duration: 4 h. Experimental Results: Dramatically suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group. |
| Animal Protocol |
Animal/Disease Models: Human hypertrophic scars were implanted in 60 nude mice[4].
Doses: 300 μg/mL was added the Lipogel. Route of Administration: Topical application daily administered. Experimental Results: Successful shedding was achieved in 83,3% of the xenografts. |
| References |
[1]. Cindy Neuzillet, et al. Targeting the TGFβ pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
[2]. Jun Yang, et al. Upregulation of microRNA‑590 in rheumatoid arthritis promotes apoptosis of bone cells through transforming growth factor‑β1/phosphoinositide 3‑kinase/Akt signaling. Int J Mol Med. 2019 May;43(5):2212-2220. [3]. Wanming He, et al. MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. Oncogene. 2019 Jun;38(23):4637-4654. [4]. Shan Shan Qiu, et al. Effect of P144® (Anti-TGF-β) in an "In Vivo" Human Hypertrophic Scar Model in Nude Mice. PLoS One. 2015 Dec 31;10(12):e0144489. [5]. Gabriel Gallo-Oller, et al. P144, a Transforming Growth Factor beta inhibitor peptide, generates antitumoral effects and modifies SMAD7 and SKI levels in human glioblastoma cell lines. Cancer Lett. 2016 Oct 10;381(1):67-75. |
| Molecular Formula |
C70H110N17O24S2F3
|
|---|---|
| Molecular Weight |
1694.84
|
| Related CAS # |
Disitertide diammonium;Disitertide;272105-42-7
|
| Solubility (In Vitro) |
H2O :< 0.1 mg/mL
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (1.48 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (1.48 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5900 mL | 2.9501 mL | 5.9003 mL | |
| 5 mM | 0.1180 mL | 0.5900 mL | 1.1801 mL | |
| 10 mM | 0.0590 mL | 0.2950 mL | 0.5900 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
