| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FXR agonist 13 (Compound E2) (24 h) exhibited potent FXR agonist activity with an EC50 of 0.097 μM and a maximum potency (Emax) of 92.4% in HEK293T cells[1]. FXR agonist 13 (20 μM, 24 h) did not significantly activate LXRα/β, PPARα/γ/δ, PXR, and TGR5 in HEK293T cells[1]. The metabolism of FXR agonist 13 (0.1 μM, 0–60 min) was mainly handled by CYP3A4/5 and CYP2C8[1].
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|---|---|
| ln Vivo |
FXR agonist 13 (Compound E2) (3-30 mg/kg, radial artery, once daily for 4 weeks) effectively improved hepatic steatosis, modulatory and fibrotic in growth and MASH models by inhibiting dye production and modulating dye [1].
|
| Animal Protocol |
Animal/Disease Models: Obesity and MASH models were induced in male C57BL/6J mice (6 weeks old, initial weight 18-22 g) by feeding them a high-fat diet (HFD, 60% of calories from fat) for 12 weeks[1].
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: P.o., once daily for 4 weeks Experimental Results: No significant improvement in body weight, but a significant decrease in liver weight ratio, indicating a reduction in liver lesions. Improved liver appearance; H&E staining showed reduced steatosis and hepatocellular damage. Significantly reduced serum ALT and AST levels(10 mg/kg). Reduced serum total cholesterol (TC) levels, but had little effect on high-density lipoprotein (HDL). Significantly reduced hepatic triglyceride (TG) and total cholesterol (TC) levels. Significantly reduced HYP content, downregulated lipogenesis-related genes (SREBP-1c and ACC-1), but did not affect FGF15 expression. |
| References |
| Molecular Formula |
C26H20CLF4N3O3
|
|---|---|
| Molecular Weight |
533.90
|
| 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 | 1.8730 mL | 9.3650 mL | 18.7301 mL | |
| 5 mM | 0.3746 mL | 1.8730 mL | 3.7460 mL | |
| 10 mM | 0.1873 mL | 0.9365 mL | 1.8730 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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