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| ln Vitro |
In MC3T3-E1 cells, disitertide (P144, 100 μg/mL) diammonium induces the expression of Bax protein while suppressing the levels of p-Akt and PI3K protein expression[2]. It is possible to suppress MSC-induced stemness and chemoresistance by targeting the TGFβ signaling system, as evidenced by the fact that disitertide (a TGF-β1 inhibitor) diammonium abrogates the MACC1-AS1 expression in GC cells[3]. In A172 and U-87 MG GBM cell lines, disitertide (10 μg/mL to 200 μg/mL) diammonium influences proliferation, promotes apoptosis, and causes anoikis[5].
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| ln Vivo |
After two weeks of treatment, doritertide (P144, topical application, 300 μg/mL) diammonium may ameliorate hypertrophic scar morphological aspects and encourage scar maturation in a nude mouse "in vivo" model[4].
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| 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 |
C68H115N19O22S2
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| Molecular Weight |
1614.88
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| Related CAS # |
Disitertide;272105-42-7;Disitertide TFA
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| Solubility (In Vitro) |
DMSO :~10 mg/mL (~6.19 mM)
H2O :~9.09 mg/mL (~5.63 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (3.10 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6192 mL | 3.0962 mL | 6.1924 mL | |
| 5 mM | 0.1238 mL | 0.6192 mL | 1.2385 mL | |
| 10 mM | 0.0619 mL | 0.3096 mL | 0.6192 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.
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