| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TGFβ1-IN-4 (peptide 27) (1-10 μM, 24-48 h) can inhibit TGF-β1-induced myofibroblast activation, fibrosis progression and epithelial-mesenchymal transition (EMT) in NIH-3T3 and HK-2 cells [1]. TGFβ1-IN-4 (0-72 h) showed strong enzymatic resistance in mouse serum [1]. Isothermal titration calorimetry showed that TGFβ1-IN-4 (1 mM) can bind to albumin [1].
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|---|---|
| ln Vivo |
Peptide 27 (0.05-1.25 mg/kg; intraperitoneal injection; daily; 7 days) can effectively alleviate renal fibrosis caused by unilateral ureteral obstruction in a mouse model of renal fibrosis [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: NIH-3T3 cells treated with TGF-β1 Tested Concentrations: 1, 2, 5, 10 μM Incubation Duration: 48 hours Experimental Results: Reduced the expression of fibronectin and α-SMA in a dose-dependent manner. Inhibited the expression of type I collagen, MMP2, and vimentin. Real-time quantitative PCR[1] Cell Types: TGF-β1 treated NIH-3T3 cells Tested Concentrations: 1, 2 μM Incubation Duration: 48 hours Experimental Experimental Results: The expression levels of fibrosis-related genes were reduced, including fibronectin, type I collagen, MMP2, vimentin, α-SMA and TGF-β1. Western Blot Analysis [1] Cell Types: HK-2 cells treated with TGF-β1 Tested Concentrations: 1, 2, 5, 10 μM Incubation Duration: 24 hours Experimental Results: Significantly inhibited the expression of fibronectin and α-SMA. Reduced the expression of type I collagen, MMP2 and vimentin, while increasing the expression of E-cadherin.
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| Animal Protocol |
Animal/Disease Models:C57BL/6J mice (male, 20-25 g)[1]
Doses: 0.05, 0.25, 1.25 mg/kg Route of Administration: Intraperitoneal injection; once daily for 7 days Experimental Results: Improved renal condition. Prevented renal inflammation and fibrosis. Reduced extracellular matrix deposition and fibrosis marker mRNA expression in a dose-dependent manner. Alleviated the progression of epithelial-mesenchymal transition (EMT). Reduced renal fibrosis induced by unilateral ureteral obstruction (UUO) in mice within a dose range of 0.05 to 1.25 mg/kg. |
| References |
| Molecular Formula |
C51H83N13O13S2
|
|---|---|
| Molecular Weight |
1150.41
|
| Sequence |
C12-{d-Asp}-His-Asn-Cys-Pro-Gln-{d-Ala}-Cys-NH2 (Hexanedithiol linker:Cys4-Cys8)C12-{d-Asp}-HNCPQ-{d-Ala}-C-NH2 (Hexanedithiol linker:Cys4-Cys8)
|
| SequenceShortening |
C12-{d-Asp}-HNCPQ-{d-Ala}-C-NH2 (Hexanedithiol linker:Cys4-Cys8)
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8693 mL | 4.3463 mL | 8.6926 mL | |
| 5 mM | 0.1739 mL | 0.8693 mL | 1.7385 mL | |
| 10 mM | 0.0869 mL | 0.4346 mL | 0.8693 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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