| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FXR regulator 1 effectively inhibited CDCA-induced FXR activation in HEK293T cells with an IC50 value of 0.70 μM[1]. FXR regulator 1 (10 μM) effectively blocked CDCA-induced recruitment of SRC1-2 coactivator peptides to purified FXR-LBD with an inhibition rate of over 90%[1]. FXR regulator 1 (1-10 μM; 24 h) acted as a selective FXR regulator in HepG2 cells, regulating bile acid and lipid metabolism genes (SHP, BSEP, SREBP-1c, CYP7A1) in a dose-dependent manner, while having no effect on gluconeogenesis genes (PEPCK, G6Pase)[1]. FXR regulator 1 (2-10 μM) activated the AMPK-ACC pathway in cultured cells in a dose-dependent manner and increased the phosphorylation levels of AMPK and ACC[1].
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|---|---|
| ln Vivo |
FXR modulator 1 (compound 4l) (25-100 mg/kg; orally; daily; 12 weeks) dose-dependently improved hepatic steatosis, ballooning degeneration, fibrosis and dyslipidemia in CDA-HFD-induced MASH mice, with a 100 mg/kg dose restoring lipid parameters to near-normal levels and reducing total NAS score to 2.2 [1].
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| Cell Assay |
Real-time quantitative PCR [1]
Cell Types: HepG2 cells Tested Concentrations: 1-10 μM Incubation Duration: 24 h Experimental Results: Both alone and in combination with CDCA downregulated the mRNA levels of SHP, BSEP, and SREBP-1c, and completely reversed CDCA-induced SREBP-1c expression at 10 μM. Compared with the solvent control group, both alone and in combination with CDCA upregulated the CYP7A1 mRNA level in a dose-dependent manner. Neither alone nor in combination with CDCA had a significant effect on the expression of gluconeogenesis genes PEPCK and G6Pase. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (male, fed CDA-HFD for 3 weeks to induce MASH before treatment)[1]
Doses: 25 mg/kg; 50 mg/kg; 100 mg/kg Route of Administration: Oral; once daily; for 12 weeks Experimental Results: The dose-dependent reduction of elevated alanine aminotransferase (ALT), aspartate aminotransferase (AST), triglycerides (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), and hepatic hydroxyproline (Hyp) levels, while increasing high-density lipoprotein cholesterol (HDL-C) levels; the 100 mg/kg dose restored lipid parameters to near-normal levels. The dose-dependent reduction of liver/body weight ratio, thereby reversing hepatomegaly. The dose-dependent reduction of macrovesicular steatosis, hepatocyte ballooning degeneration, lipid droplet accumulation, and collagen deposition in the liver. The total NAS score decreased from 5.4 (model group) to 3.6 (25 mg/kg), 3.1 (50 mg/kg), and 2.2 (100 mg/kg); and the subscores of hepatocellular ballooning degeneration and steatosis were reduced in a dose-dependent manner. |
| References |
| Molecular Formula |
C25H20O6
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|---|---|
| Molecular Weight |
416.42
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
COC1=CC=CC(CC2=COC3=C(C2=O)C=CC(OCC4=CC=C(C=C4)C(O)=O)=C3)=C1
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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 | 2.4014 mL | 12.0071 mL | 24.0142 mL | |
| 5 mM | 0.4803 mL | 2.4014 mL | 4.8028 mL | |
| 10 mM | 0.2401 mL | 1.2007 mL | 2.4014 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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