| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
VDR agonist 4 (compound B15) (0.1 μM, 48 hours) downregulated the expression of 991 differentially expressed genes (DEGs) in LX-2 cells, upregulated the expression of 249 DEGs, and increased the expression of CYP24A1[1]. VDR agonist 4 has good safety, with no significant cytotoxicity to LX-2 cells (IC50 > 50 μM), and the hERG-mediated cardiotoxicity is negligible (IC50 > 30 μM)[1]. VDR agonist 4 (0.1 μM, 24 hours) significantly inhibited the expression of COL1A1, ACTA2 and type I collagen in LX-2 cells, and this inhibitory effect disappeared after VDR depletion, indicating that its strong anti-fibrotic activity is strictly dependent on VDR[1]. VDR agonist 4 (0.1 μM, 48 hours) downregulated the core profibrotic pathway (TGFβ/SMAD3, PEGF, JAK) and collagen synthesis genes (COL1A2, COL3A1) in LX-2 cells, while upregulating collagen degradation genes (MMP1, MMP3), thus confirming that it has the effect of inhibiting collagen production and promoting collagen degradation [1].
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|---|---|
| ln Vivo |
VDR agonist 4 (500 μg/kg, surface, 5 times a week, effective for 2 weeks) can alleviate key responses and fibrotic remodeling in CCI4-induced liver fibrosis [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: LX-2 cells Tested Concentrations: 0.1 μM Incubation Duration: 24 h Experimental Results: Significantly suppressed the production of α-SMA and collagen I. Its inhibitory effect was abolished upon VDR depletion. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (8 weeks old) intraperitoneally injected with CCl4/corn oil (1/50, v/v) mixture at a dose of 0.5 mL/kg three times a week for 4 weeks[1]
Doses: 500 μg/kg Route of Administration: p.o., five times weekly for 2 weeks Experimental Results: Exhibited potent inhibitory effects on target gene expression (Fn, Ctgf, Timp-1), with efficacy comparable to Calcipotriol. Resulted in marked attenuation of hepatic inflammation and significant amelioration of fibrotic lesions, as evidenced by reduced inflammatory markers and collagen accumulation. Resulted in a significant decrease in ALT, AST, and TBA levels. Did not result in increased serum calcium levels. |
| References |
| Molecular Formula |
C27H37NO6
|
|---|---|
| Molecular Weight |
471.59
|
| Appearance |
Typically exists as solids at room temperature
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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)
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| 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 | 2.1205 mL | 10.6024 mL | 21.2049 mL | |
| 5 mM | 0.4241 mL | 2.1205 mL | 4.2410 mL | |
| 10 mM | 0.2120 mL | 1.0602 mL | 2.1205 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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