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| Targets |
β-FXR antagonist 1 targets the farnesoid X receptor (FXR), a nuclear receptor that regulates bile acid synthesis, lipid metabolism, and glucose homeostasis. FXR is activated by bile acids and plays a critical role in maintaining metabolic balance. Antagonism of FXR can modulate bile acid and lipid metabolism, making it a potential therapeutic target for metabolic diseases such as non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and cholestatic liver diseases.
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| ln Vitro |
In vitro, β-FXR antagonist 1 inhibits FXR-mediated signaling pathways. The compound's activity is measured using cell-based reporter assays where FXR activation is monitored by luciferase activity driven by FXR response elements. β-FXR antagonist 1 can also be assessed for its ability to modulate the expression of FXR target genes such as small heterodimer partner (SHP) and bile salt export pump (BSEP) in hepatocytes. Its selectivity as an antagonist distinguishes it from agonists that activate FXR.
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| ln Vivo |
In vivo, β-FXR antagonist 1 has potential applications in studying metabolic diseases and liver function. By inhibiting FXR, the compound can modulate bile acid and lipid metabolism in animal models. Detailed in vivo efficacy data, including effects on bile acid levels, lipid profiles, and liver histology in models of NAFLD, NASH, or cholestasis, are described in the primary literature. The compound's isomer status may provide a differentiated profile compared to other FXR antagonists.
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| Enzyme Assay |
Non-cellular binding assays for β-FXR antagonist 1 involve measuring its binding affinity to FXR using techniques such as fluorescence polarization, scintillation proximity assays, or surface plasmon resonance. The compound's ability to antagonize FXR can be assessed in cell-free systems using purified FXR protein and coactivator peptides in the presence of an FXR agonist. Antagonism is confirmed by the compound's ability to inhibit agonist-induced FXR activation in biochemical assays.
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| Cell Assay |
In vitro cellular experiments with β-FXR antagonist 1 are conducted in hepatocyte cell lines or other cell types expressing FXR. Cells are treated with the compound in the presence or absence of FXR agonists (e.g., chenodeoxycholic acid or GW4064). FXR transcriptional activity is measured using luciferase reporter assays containing FXR response elements. The expression of FXR target genes is assessed by qPCR. Cell viability and cytotoxicity are evaluated using standard assays.
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| Animal Protocol |
In vivo animal studies for β-FXR antagonist 1 are performed in mouse or rat models of metabolic diseases such as NAFLD, NASH, or cholestasis. Animals are treated with the compound via appropriate routes of administration. Endpoints include measurements of bile acid levels, lipid profiles (triglycerides, cholesterol), liver enzymes (ALT, AST), and histopathological assessment of liver tissue. The compound's effects on FXR target gene expression in the liver are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of β-FXR antagonist 1 include a molecular formula of C36H59NO5 and a molecular weight of 585.86. The CAS number is 2295804-92-9. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in appropriate animal models. Storage conditions should follow the supplier's recommendations. The compound is for research use only and is not for human therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicity data for β-FXR antagonist 1 are generated during preclinical development. As an FXR modulator, potential toxicities may include effects on bile acid homeostasis and liver function. Comprehensive toxicology studies would assess safety margins and identify target organ toxicities. Researchers should consult the safety data sheet and handle the compound with appropriate laboratory safety precautions for research use only.
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| References | |
| Additional Infomation |
β-FXR antagonist 1 (C 12) is an isomer of FXR antagonist 1). It is a selective FXR antagonist. The compound is valuable for research on metabolic diseases and liver function. All products are for research use only and not for human therapeutic applications.
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| CAS # |
2295804-92-9
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| Appearance |
White to off-white solid powder
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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) |
Typically soluble in DMSO (e.g. 10 mM)
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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.) |
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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