| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TGF-beta1 (transforming growth factor-beta 1) and PI3K (phosphoinositide 3-kinase).
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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].
In MC3T3-E1 cells at 100 microg/mL, induces Bax expression while suppressing p-Akt and PI3K protein expression; in GC cells, abrogates MACC1-AS1 expression; in A172 and U-87 MG GBM cells at 10-200 microg/mL, influences proliferation, promotes apoptosis, and causes anoikis. |
| 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].
Topical application at 300 microg/mL (Lipogel formulation) for two weeks in a nude mouse xenograft model of human hypertrophic scars improves scar morphology and promotes maturation, with 83.3% of xenografts achieving successful shedding. |
| Enzyme Assay |
Binding affinity is typically assessed by surface plasmon resonance (SPR) or competitive ELISA using immobilized TGF-beta1 receptor or biotinylated TGF-beta1; peptide-resin binding experiments quantify direct receptor-ligand interaction blockage.
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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. MC3T3-E1 cells (mouse embryo osteoblast precursors) are treated with 100 microg/mL for 4 hours; cells are then lysed and subjected to Western blotting with antibodies against PI3K, p-Akt, and Bax. |
| 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. Human hypertrophic scar tissues are implanted into 60 nude mice; after engraftment, 300 microg/mL Disitertide in Lipogel is applied topically daily; scar morphology and maturation are assessed histologically after two weeks. |
| ADME/Pharmacokinetics |
PK properties are not extensively reported for the diammonium salt; as a peptide, typical bioavailability is low via oral administration, requiring topical or injectable routes for efficacy.
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| Toxicity/Toxicokinetics |
Toxicity studies for this specific diammonium salt are not detailed; however, as an investigational peptide, standard safety pharmacology and toxicology studies would be required for clinical development.
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| References | |
| Additional Infomation |
Disitertide is under investigation for fibrotic diseases and dermal scarring; it has not received regulatory approval and is currently only available for non-clinical research applications.
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| 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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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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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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