| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TGF-β1/Smad3-IN-1 (100-500 nM; 48 h) leads to a decrease in TGF-β1 levels in H2228 cells, showing a better inhibitory effect than Nintedanib (HY-50904) at the same concentration [1]. TGF-β1/Smad3-IN-1 (2-6 μM; 24 h) exhibits a dose-dependent inhibition of p-Smad3 and α-SMA expression, and significantly inhibits NIH3T3 cell migration [1]. TGF-β1/Smad3-IN-1 (3-10 μM; 72 h) increases the expression of Cleave-casepase3 in NIH3T3 cells, and induces cell apoptosis in a dose-dependent manner [1]. The IC50 of TGF-β1/Smad3-IN-1 for NIH3T3 cells is 1.07 μM. The IC50 for TGFβ1-activated HFL1 cells was 2.86 ± 0.014 μM. It effectively inhibited the expression of activation marker α-SMA[1]. Apoptosis Analysis[1] Cell Line: NIH3T3 Concentration: 3, 7.5, 10 μM Incubation Time: 72 h Result: At the highest concentration of 10 μM, the total apoptosis rate of cells reached 91.79%, indicating that 5aa has a strong ability to induce apoptosis.
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|---|---|
| ln Vivo |
The bioavailability of TGF-β1/Smad3-IN-1 in SD rats is higher than that of Nintedanib (HY-50904)[1]. TGF-β1/Smad3-IN-1 (po; 100 mg/kg/; from the second to the twentieth day) can inhibit the expression of bleomycin-induced lung TGFβ1 and HYP, reduce extracellular matrix deposition, and alleviate lung fibrosis in the mouse pulmonary fibrosis model induced by bleomycin[1].
|
| Animal Protocol |
Animal/Disease Models:Bleomycin-induced model of pulmonary fibrosis in mice[1]
Doses: 100 mg/kg/ Route of Administration: p.o.; day 2-20 Experimental Results: Significantly reduced α-SMA, fibronection and p-smad3 protein expression levels. Significantly reduced TGFβ1 levels, more effective than Nintedanib. Reduced hydroxyproline (HYP) levels. |
| References |
| Molecular Formula |
C30H34N4O6S
|
|---|---|
| Molecular Weight |
578.68
|
| Appearance |
Light yellow to yellow 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 |
| 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 | 1.7281 mL | 8.6404 mL | 17.2807 mL | |
| 5 mM | 0.3456 mL | 1.7281 mL | 3.4561 mL | |
| 10 mM | 0.1728 mL | 0.8640 mL | 1.7281 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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