| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TGF-β1/Smad3-IN-2 (compound D13) (0.1 μM; 24 h) significantly downregulated the expression of type I collagen (COL1A1) and α-SMA (ACTA2) in TGF-β1-induced human LX-2 hepatic stellate cells (HSCs) [1]. TGF-β1/Smad3-IN-2 showed very low cytotoxicity to the human hepatic stellate cell line LX-2, with an IC50 > 50 μM [1]. TGF-β1/Smad3-IN-2 (0.1 μM; 48 h) induced the downregulation of 654 differentially expressed genes and the upregulation of 507 differentially expressed genes in the TGF-β1-stimulated human hepatic stellate cell line LX-2, among which the core fibrosis genes (COL1A1, COL1A2, COL3A1) were significantly downregulated and significantly enriched in the TGF-β signaling pathway, ECM-receptor interaction pathway and Hippo signaling pathway [1]. TGF-β1/Smad3-IN-2 promotes direct interaction between VDR and SMAD3 proteins in human hepatic stellate cell line LX-2[1].
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|---|---|
| ln Vivo |
TGF-β1/Smad3-IN-2 (100 μg/kg; oral gavage; once daily for 2 weeks) showed antifibrotic efficacy in a mouse model of liver fibrosis induced by bile duct ligation [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: LX-2 human hepatic stellate cells (HSC) Tested Concentrations: 0.1 μM Incubation Duration: 24 hours Experimental Results: α-SMA and type I collagen levels were reduced to near baseline levels. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (male, 8 weeks old, bile duct ligation induced liver fibrosis) [1]
Doses: 100 μg/kg Route of Administration: Gavage; once daily for 2 weeks Experimental Results: Significantly reduced liver inflammation and decreased collagen accumulation in liver tissue, with efficacy comparable to calcipotriol. Significantly downregulated the expression of pro-fibrotic genes Ctgf, Fn, and Timp-1 in the liver. Significantly reduced serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bile acid (TBA) levels. No significant changes in serum calcium levels. |
| References |
| Molecular Formula |
C38H47NO3
|
|---|---|
| Molecular Weight |
565.78
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(N(CC1=CC=CC=C1)CC2=CC=CC=C2)/C=C/[C@H]([C@H]3CC[C@H]([C@]3(C)CCC/4)C4=C\C=C(C[C@@H](O)C[C@@H]5O)/C5=C)C
|
| 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 | 1.7675 mL | 8.8374 mL | 17.6747 mL | |
| 5 mM | 0.3535 mL | 1.7675 mL | 3.5349 mL | |
| 10 mM | 0.1767 mL | 0.8837 mL | 1.7675 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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