| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Targets |
The primary molecular target of 4'-Methoxychalcone is the Peroxisome Proliferator-Activated Receptor gamma (PPARγ). It functions as a selective modulator of PPARγ, activating this nuclear receptor. By activating PPARγ, 4'-Methoxychalcone regulates adipocyte differentiation and modulates the expression and secretion of a variety of adipokines in adipose tissue that are involved in insulin sensitivity. PPARγ is a key transcription factor that controls the expression of genes involved in lipid metabolism, glucose homeostasis, and inflammation. The compound's activation of PPARγ leads to the increased expression of adipogenic genes, contributing to its effects on adipocyte biology. Unlike some full PPARγ agonists, 4'-Methoxychalcone may offer a more selective modulation of the receptor, potentially reducing side effects associated with full agonists.
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| ln Vitro |
4'-Methoxychalcone (5 μM; 8 days) increases during adipocyte differentiation the mRNA expression of adipogenic genes, PPARγ, aP2, FAS, adiponectin, and GluT 4 substantially [1]. In preadipocyte 3T3-L1 cells, 4'-Methoxychalcone (5 μM; 8 days) decreases TNF-α-upregulated IL-6, PAI-1, and MCP-1 mRNA expression [1]. Increased PPARγ expression is caused during differentiation by 4'-Methoxychalcone (5 μM; 0-8 days), although C/EBPβ protein expression is mostly unaffected [1].
In vitro, 4'-Methoxychalcone demonstrates potent activity in regulating adipocyte differentiation. At a concentration of 5 μM over 8 days, it substantially increases the mRNA expression of key adipogenic genes, including PPARγ, aP2 (fatty acid-binding protein 4), FAS (fatty acid synthase), adiponectin, and Glut4 (glucose transporter type 4) in 3T3-L1 preadipocytes. The compound also decreases the TNF-α-upregulated mRNA expression of pro-inflammatory adipokines such as IL-6, PAI-1, and MCP-1 in these cells. This indicates that 4'-Methoxychalcone not only promotes adipocyte differentiation but also exerts an anti-inflammatory effect on adipose tissue, improving the overall adipokine profile. The increased PPARγ expression during differentiation is a key event, while the expression of C/EBPβ, another important transcription factor, remains largely unaffected, suggesting a specific mechanism of action. |
| ln Vivo |
In vivo, the primary effects of 4'-Methoxychalcone are related to its role as a PPARγ agonist. Based on its in vitro activity, the compound is expected to have therapeutic potential for improving insulin sensitivity and managing metabolic disorders such as type 2 diabetes. By modulating the expression and secretion of adipokines in adipose tissue, it may help to reduce chronic low-grade inflammation associated with obesity and insulin resistance. However, detailed in vivo efficacy data, such as its effects on blood glucose levels, insulin sensitivity, and lipid profiles in animal models of diabetes or obesity, are not extensively documented in the public literature. Further in vivo studies are required to fully characterize its therapeutic potential and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro PPARγ binding assays, 4'-Methoxychalcone can be evaluated using commercially available PPARγ ligand-binding domain (LBD) kits. These assays typically involve incubating the PPARγ LBD with a fluorescent or radiolabeled known ligand (e.g., rosiglitazone) and varying concentrations of the test compound. The displacement of the tracer ligand is measured to determine the binding affinity (IC50 or Ki). Alternatively, cell-based reporter gene assays can be used, where cells are transfected with a PPARγ expression plasmid and a luciferase reporter gene driven by a PPAR response element (PPRE). The compound's ability to activate the receptor is measured by the increase in luciferase activity.
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| Cell Assay |
RT-PCR[1]
Cell Types: Preadipocyte 3T3-L1 Cell Tested Concentrations: 5 μM Incubation Duration: 0 days; 2 days; 4 days; 6 days; 8 days Experimental Results: All adipogenic genes in adipocytes except GluT1 mRNA expression was increased. Western Blot Analysis[1] Cell Types: Preadipocyte 3T3-L1 Cell Tested Concentrations: 5 μM Incubation Duration: 8 days Experimental Results: PPARγ expression increased in adipocytes. For in vitro cell-based assays, the most common model is the mouse 3T3-L1 preadipocyte cell line. Cells are cultured in Dulbecco's Modified Eagle Medium (DMEM) supplemented with fetal bovine serum. Differentiation is induced using a standard cocktail (e.g., insulin, dexamethasone, and IBMX). 4'-Methoxychalcone is typically tested at a concentration of 5 μM and added to the differentiation medium for 8 days. On day 8, cells are harvested for RNA extraction and quantitative RT-PCR analysis to measure the expression of adipogenic and adipokine genes. Alternatively, cells can be processed for Western blotting to analyze protein expression, such as PPARγ and C/EBPβ. Oil Red O staining can also be performed to visualize and quantify lipid accumulation, a hallmark of adipocyte differentiation. |
| Animal Protocol |
For in vivo animal studies, 4'-Methoxychalcone is typically administered orally or intraperitoneally in rodent models. To study its effects on metabolism and insulin sensitivity, C57BL/6 mice can be fed a high-fat diet to induce obesity and insulin resistance. The compound is then administered daily for several weeks. Parameters such as body weight, food intake, and blood glucose levels are monitored. Glucose tolerance tests (GTT) and insulin tolerance tests (ITT) are performed to assess insulin sensitivity. At the end of the study, adipose tissue, liver, and muscle are collected for histology and gene expression analysis. Blood samples are analyzed for insulin, lipid profiles, and adipokine levels.
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| ADME/Pharmacokinetics |
Physicochemical properties of 4'-Methoxychalcone: Molecular Formula C16H14O2, Molecular Weight 238.28, LogP 3.591. It is soluble in DMSO and ethanol but practically insoluble in water. As a small, lipophilic molecule, it is expected to have good oral absorption. However, detailed pharmacokinetic parameters such as Cmax, Tmax, half-life, and bioavailability are not available in the public literature. Further studies are required to determine its metabolic stability and tissue distribution.
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| Toxicity/Toxicokinetics |
Specific toxicity data for 4'-Methoxychalcone are limited. Based on its structural class as a chalcone and its use in research, it is generally handled with standard laboratory safety precautions. Comprehensive toxicological studies, including acute and chronic toxicity, genotoxicity, and carcinogenicity assessments, have not been published. The compound is not intended for human use and is for research purposes only.
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| References | |
| Additional Infomation |
4'-Methoxychalcone is a member of the chalcone class of compounds.
4'-Methoxychalcone is a research compound with no clinical trial or regulatory approval status. It is commercially available from chemical suppliers for research purposes only. Its primary value lies in its use as a pharmacological tool to study PPARγ-mediated signaling pathways, adipocyte differentiation, and insulin sensitivity. It is also used in studies investigating the anti-inflammatory and anti-tumor activities of chalcones. The compound is not approved for human therapeutic use. |
| Molecular Formula |
C16H14O2
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| Molecular Weight |
238.28116
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| Exact Mass |
238.099
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| CAS # |
959-23-9
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| PubChem CID |
641818
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| Appearance |
White to light yellow solid powder
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| Density |
1.114g/cm3
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| Boiling Point |
397.5ºC at 760mmHg
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| Melting Point |
107 °C
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| Flash Point |
180.5ºC
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| Index of Refraction |
1.606
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| LogP |
3.591
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
282
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)C(=O)/C=C/C2=CC=CC=C2
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| InChi Key |
KJHHAPASNNVTSN-KPKJPENVSA-N
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| InChi Code |
InChI=1S/C16H14O2/c1-18-15-10-8-14(9-11-15)16(17)12-7-13-5-3-2-4-6-13/h2-12H,1H3/b12-7+
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| Chemical Name |
(E)-1-(4-methoxyphenyl)-3-phenylprop-2-en-1-one
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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) |
DMSO : ~50 mg/mL (~209.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1967 mL | 20.9837 mL | 41.9674 mL | |
| 5 mM | 0.8393 mL | 4.1967 mL | 8.3935 mL | |
| 10 mM | 0.4197 mL | 2.0984 mL | 4.1967 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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