| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
DiMNF targets the aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor that mediates the toxic and biological effects of environmental pollutants such as dioxins. AhR is involved in xenobiotic metabolism, immune regulation, and cell proliferation. DiMNF is a competitive AhR ligand with significant antagonistic activity (IC50 = 21 nM), meaning it binds to AhR and blocks the activation of AhR-mediated gene expression by agonists. It has anti-inflammatory activity.
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| ln Vitro |
There is little effect of DiMNF (3',4'-Dimethoxy-αNF) (10 μM; 4 h) on the AHR genome [1]. DiMNF (10 μM; 1 hour) efficiently suppresses the expression of inflammatory genes mediated by cytokines [1]. Within AHR's ligand-binding pocket, DiMNF takes on a distinct orientation [1].
In vitro, DiMNF is a selective AhR modulator with an IC50 of 21 nM. It has anti-inflammatory activity and inhibits cytokine-mediated complement factor gene induction. The compound's potent AhR antagonism makes it a valuable tool for studying the role of AhR in inflammation, immune regulation, and xenobiotic metabolism. It can be used to investigate the effects of AhR inhibition on gene expression, cell proliferation, and inflammatory responses. |
| ln Vivo |
In vivo, DiMNF has potential applications in studying AhR-mediated inflammation and immune regulation. By inhibiting AhR, the compound may reduce inflammation and modulate immune responses. However, specific in vivo efficacy data for DiMNF have not been detailed in the available literature. The compound has been studied in the context of cancer research. Further preclinical studies would be required to assess its therapeutic potential.
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| Enzyme Assay |
For receptor binding assays, cells expressing AhR or AhR protein preparations are incubated with radiolabeled ligands (such as [³H]TCDD) at various concentrations of DiMNF (typically 0.001-100 µM) in binding buffer. Nonspecific binding is determined in the presence of excess unlabeled ligand. Bound radioligand is separated, and radioactivity is quantified. IC50 values for competition binding are calculated.
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| Cell Assay |
RT-PCR[1]
Cell Types: Huh7 Cell Tested Concentrations: 10 μM Incubation Duration: 4 hrs (hours) or 1 hour Experimental Results: diminished CYP1A1 mRNA expression (4 hrs (hours)). Exhibits inhibitory activity on cytokine-mediated induction of SAA1 (1 hour). Dramatically diminished IL1β-mediated induction of C4, C1S, C1R and C3 mRNA. For reporter gene assays, cells are transfected with an AhR-responsive luciferase reporter construct (such as the DRE-luciferase reporter) and treated with DiMNF alone or in combination with AhR agonists (such as TCDD). After incubation, luciferase activity is measured. The compound's ability to inhibit agonist-induced reporter activity is quantified, and IC50 values are calculated. For anti-inflammatory assays, cells are treated with DiMNF and inflammatory stimuli, and cytokine production is measured by ELISA. |
| Animal Protocol |
For in vivo studies, animal models of inflammation would be used to evaluate the anti-inflammatory activity of DiMNF. Mice would be administered DiMNF via oral or intraperitoneal routes at doses determined from pharmacokinetic studies. Inflammatory markers, cytokine levels, and AhR target gene expression would be assessed in tissues. However, specific in vivo protocols for DiMNF have not been detailed in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DiMNF have not been fully characterized in the available literature. The compound has a molecular weight of 332.35 g/mol, suggesting potential for drug-like properties. It is soluble in DMSO (1.5 mg/mL). Standard PK studies including half-life, bioavailability, and tissue distribution would be required for in vivo studies. The compound is typically stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for DiMNF have not been reported. As a research compound, it is intended for laboratory use only and is not for human or veterinary use. Standard safety precautions should be followed when handling this compound. Comprehensive toxicology studies would be required before any clinical development.
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| References | |
| Additional Infomation |
DiMNF (3′,4′-Dimethoxy-α-naphthoflavone) is a selective aryl hydrocarbon receptor (AhR) modulator (SAhRM). It is a competitive AhR ligand with IC50 of 21 nM. DiMNF has anti-inflammatory activity and inhibits cytokine-mediated complement factor gene induction. It is used as a research tool for studying AhR biology. DiMNF is not approved for clinical use.
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| Molecular Formula |
C21H16O4
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|---|---|
| Molecular Weight |
332.34934
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| Exact Mass |
332.105
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| CAS # |
14756-24-2
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| PubChem CID |
276138
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.271g/cm3
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| Boiling Point |
513.8ºC at 760 mmHg
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| Flash Point |
227.3ºC
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| Vapour Pressure |
1.15E-10mmHg at 25°C
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| Index of Refraction |
1.65
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| LogP |
4.63
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
528
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QDZQDIUUJDAORK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16O4/c1-23-18-10-8-14(11-20(18)24-2)19-12-17(22)16-9-7-13-5-3-4-6-15(13)21(16)25-19/h3-12H,1-2H3
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| Chemical Name |
2-(3,4-dimethoxyphenyl)benzo[h]chromen-4-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 : ~12.5 mg/mL (~37.61 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0089 mL | 15.0444 mL | 30.0888 mL | |
| 5 mM | 0.6018 mL | 3.0089 mL | 6.0178 mL | |
| 10 mM | 0.3009 mL | 1.5044 mL | 3.0089 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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