| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
RXR antagonist 5 selectively targets the retinoic acid X receptor (RXR), a member of the nuclear receptor superfamily. As an antagonist, it binds to RXR and blocks its activation by endogenous ligands (9-cis retinoic acid). RXR forms heterodimers with other nuclear receptors (such as PPAR, LXR, FXR, RAR, and VDR) and plays a critical role in regulating gene expression involved in metabolism, cell differentiation, and inflammation. By antagonizing RXR, this compound disrupts the activity of multiple RXR heterodimers.
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| ln Vitro |
Specific in vitro activity data for RXR antagonist 5 is not provided in the search results. However, as a selective RXR antagonist, it would be expected to inhibit RXR-mediated transcriptional activity in cell-based reporter assays. The binding potential was evaluated by modeling, suggesting its affinity was predicted computationally. The compound is designed to effectively disrupt RXR signaling pathways.
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| ln Vivo |
Specific in vivo activity data for RXR antagonist 5 is not provided. As a research tool for studying RXR signaling, it would be used in animal models of metabolic diseases, dermatological conditions, and cancer. RXR antagonists have been shown to modulate glucose and lipid metabolism, inhibit tumor growth, and affect differentiation processes. However, no specific animal data for this compound is reported.
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| Enzyme Assay |
The binding affinity of RXR antagonist 5 for RXR can be determined by a competition binding assay using radiolabeled 9-cis retinoic acid. Procedure: Recombinant human RXRalpha protein (10 nM) is incubated with varying concentrations of RXR antagonist 5 (0.1-1000 nM) and 5 nM [3H]-9-cis retinoic acid in binding buffer (10 mM Tris-HCl, pH 8.0, 100 mM KCl, 1 mM DTT, 5% glycerol) for 16-20 hours at 4degC. Unbound ligand is removed by charcoal-dextran adsorption, followed by centrifugation. The supernatant containing bound ligand is counted by scintillation. The IC50 is calculated, and the Ki is derived using the Cheng-Prusoff equation.
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| Cell Assay |
The transcriptional activity of RXR antagonist 5 can be assessed in a cell-based reporter assay. Procedure: HEK293T cells are seeded in 96-well white plates (1×10⁴ cells/well) and co-transfected with a plasmid expressing human RXRalpha, a luciferase reporter gene driven by a retinoic acid response element (RARE), and a Renilla luciferase control for normalization. After 24 hours, cells are treated with varying concentrations of RXR antagonist 5 (0.1-1000 nM) in the presence of 100 nM 9-cis retinoic acid (full agonist) for 24 hours. Firefly and Renilla luciferase activities are measured using the Dual-Luciferase Reporter Assay System. The IC50 is calculated as the concentration that inhibits 50% of the 9-cis retinoic acid-induced luciferase activity.
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| Animal Protocol |
In vivo efficacy can be evaluated in a mouse model of type 2 diabetes (db/db mice). Procedure: Male db/db mice (8 weeks, n=10 per group) are administered RXR antagonist 5 orally at doses of 10, 30, and 100 mg/kg once daily for 4 weeks. Control groups receive vehicle or the RXR agonist bexarotene (10 mg/kg). Blood glucose and body weight are measured weekly. An oral glucose tolerance test (OGTT) is performed at week 2. At study endpoint, mice are euthanized, and blood is collected for serum insulin, triglycerides, and cholesterol levels. Liver and adipose tissue are harvested for histological analysis and gene expression studies of RXR target genes (e.g., PEPCK, ApoE).
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| ADME/Pharmacokinetics |
Specific PK data for RXR antagonist 5 is not provided. As a small molecule with a molecular weight of 366.50 g/mol, it is expected to have good oral bioavailability. The compound's molecular formula (C23H30N2O2) indicates it has moderate lipophilicity, which is favorable for membrane permeability. For in vivo studies, it is likely formulated in a vehicle such as 0.5% methylcellulose or DMSO:PEG300:saline. The compound is stored at -20degC under recommended conditions.
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| Toxicity/Toxicokinetics |
Specific toxicology data for RXR antagonist 5 is not available. As a selective RXR antagonist, potential toxicities may include metabolic disturbances and alterations in cell differentiation. RXR agonists like bexarotene are known to cause hyperlipidemia and hypothyroidism. An antagonist may have different safety profiles. Standard safety precautions for handling research chemicals should be followed.
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| References | |
| Additional Infomation |
RXR antagonist 5 (compound 22, V-125) is a selective antagonist of the retinoic acid X receptor (RXR). RXR is a nuclear receptor that heterodimerizes with other nuclear receptors such as PPAR, LXR, FXR, RAR, and VDR, serving as a master regulator of metabolic and differentiation pathways. By antagonizing RXR, this compound can inhibit the activity of multiple downstream pathways simultaneously. It is a valuable research tool for studying the role of RXR in metabolic diseases, cancer, and inflammation. This product is for research use only and is not an approved drug.
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| Molecular Formula |
C23H30N2O2
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|---|---|
| Molecular Weight |
366.50
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| CAS # |
1807740-94-8
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| 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 | 2.7285 mL | 13.6426 mL | 27.2851 mL | |
| 5 mM | 0.5457 mL | 2.7285 mL | 5.4570 mL | |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7285 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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