| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
VDR agonist 5 (compound II-8) (0.5 μM) acts as a VDR agonist in the human hepatic stellate cell line LX-2 and significantly upregulates the expression level of the VDR target gene CYP24A1 [1]. VDR agonist 5 (0.01-1 μM; 48 h) activates VDR-mediated transcription in HEK293 cells, showing significant transcriptional activation activity at 0.5 μM and a dose-dependent response in the concentration range of 0.01, 0.1 and 1 μM [1]. VDR agonist 5 (II-8) (0.5 μM; 24 h) inhibits TGF-β1-induced activation of the human hepatic stellate cell line LX-2, significantly reduces the mRNA and protein expression levels of profibrotic markers α-SMA and type I collagen, and its activity lasts for at least 48 hours [1]. VDR agonist 5 (0.5 μM; 24 h) has antifibrotic activity and specifically inhibits TGF-β1-induced activation of LX-2 human hepatic stellate cells. This effect is mediated by the vitamin D receptor, as VDR knockdown significantly weakens its ability to inhibit α-SMA and type I collagen expression [1].
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|---|---|
| ln Vivo |
VDR agonist 5 (compound II-8) (500 μg/kg; orally; daily; 7 days) significantly reduced BDL-induced liver fibrosis and restored liver function in male C57BL/6 mice without causing hypercalcemia [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: TGF-β1-activated LX-2 human hepatic stellate cell line Tested Concentrations: 0.5 μM Incubation Duration: 24 hours (after siRNA transfection, TGF-β1 was activated simultaneously) Experimental Results: Compared with cells treated with TGF-β1 alone, the upregulation of TGF-β1-induced α-SMA and type I collagen expression in siNC transfected cells was significantly reduced. Compared with siNC transfected cells treated with target reagent and TGF-β1, the ability of siVDR transfected cells to reduce α-SMA and type I collagen expression was significantly weakened, and the protein levels were significantly increased. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (male, 8 weeks old, bile duct ligation-induced liver fibrosis) [1]
Doses: 500 μg/kg Route of Administration: Oral; once daily for 7 days Experimental Results: Significantly reduced fibrotic lesions and decreased type I collagen deposition (comparable to the positive control calcipotriol). Significantly downregulated the mRNA expression of liver fibrosis-related genes Timp-1, CTGF, and Fn. Significantly reduced the protein levels of hepatic α-SMA, CTGF, and fibronectin. Significantly reduced serum ALT, AST, and TBA levels. Did not induce hypercalcemia (serum calcium levels were comparable to the control group and untreated bile duct ligation mice). |
| References |
| Molecular Formula |
C30H42N2O5
|
|---|---|
| Molecular Weight |
510.66
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC2=C(C=C1)C(C(CC)(C3=CC=C(OCC(O)CO)C=C3)CC)=CN2CC)NC(C(C)C)CO
|
| 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 | 1.9583 mL | 9.7913 mL | 19.5825 mL | |
| 5 mM | 0.3917 mL | 1.9583 mL | 3.9165 mL | |
| 10 mM | 0.1958 mL | 0.9791 mL | 1.9583 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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