| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Aryl Hydrocarbon Receptor (AhR). CHD-5 is a potent antagonist of AhR, blocking the activation of AhR-mediated signaling pathways.
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| ln Vitro |
In vitro, CHD-5 acts as a potent AhR antagonist, inhibiting AhR-mediated transcriptional activity. The compound binds to AhR and prevents its activation by endogenous or exogenous ligands, thereby blocking downstream gene expression. CHD-5 is used in cellular studies to investigate the role of AhR in various biological processes, including immune regulation and cancer biology.
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| ln Vivo |
In vivo activity of CHD-5 has not been extensively characterized. As an AhR antagonist, it is expected to modulate AhR-dependent physiological processes such as xenobiotic metabolism, immune responses, and developmental signaling. Further pharmacokinetic and pharmacodynamic studies are required to establish in vivo efficacy.
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| Enzyme Assay |
Non-cell receptor binding assays for CHD-5 are performed using membrane preparations or purified AhR protein. Radioligand binding studies are conducted using [³H]TCDD or [³H]FICZ as tracers. AhR protein is incubated with the radioligand and varying concentrations of CHD-5 (0.001-100 μM). Nonspecific binding is determined with excess unlabeled TCDD. After incubation at 25°C for 60-120 minutes, bound and free ligand are separated by filtration or charcoal adsorption, and radioactivity is counted. IC₅₀ and Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays for CHD-5 are performed using cell lines expressing AhR, such as HepG2 hepatoma cells or mouse embryonic fibroblasts. Cells are treated with CHD-5 at concentrations ranging from 0.01-100 μM in the presence or absence of AhR agonists (e.g., TCDD or FICZ). AhR transcriptional activity is measured using luciferase reporter assays (e.g., XRE-luciferase). CYP1A1 expression is quantified by qPCR or Western blotting as a marker of AhR activation. IC₅₀ values for inhibition of AhR activity are calculated from dose-response curves.
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| Animal Protocol |
In vivo studies for CHD-5 would typically involve mouse models of inflammation, cancer, or developmental biology. CHD-5 would be administered via intraperitoneal or oral routes at doses determined from pharmacokinetic studies. AhR target gene expression in tissues (e.g., liver, lung, intestine) would be assessed by qPCR. Disease severity, inflammatory cytokine levels, and tissue histopathology would be evaluated. However, detailed published in vivo protocols for CHD-5 are currently limited.
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| ADME/Pharmacokinetics |
Published pharmacokinetic data for CHD-5 are limited. The compound has a molecular weight of 319.36 and a molecular formula of C19H17N3O2. It is typically stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 6 months. CHD-5 is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for CHD-5 are not available in the public domain. No significant toxicity has been reported at effective concentrations in vitro. Standard safety pharmacology studies would be required for therapeutic development. The compound is for research use only.
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| References | |
| Additional Infomation |
CHD-5 is a potent aryl hydrocarbon receptor (AhR) antagonist. AhR is a ligand-activated transcription factor involved in xenobiotic metabolism, immune regulation, and cellular differentiation. CHD-5 is used as a research tool to study AhR signaling pathways and their role in inflammation and cancer. It is not approved for clinical use.
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| Molecular Formula |
C19H17N3O2
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|---|---|
| Molecular Weight |
319.36
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| Exact Mass |
319.132
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| CAS # |
289494-16-2
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| PubChem CID |
2827423
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| Appearance |
Yellow to orange solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
426.9±45.0 °C at 760 mmHg
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| Flash Point |
212.0±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.612
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| LogP |
5.49
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
454
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RDQWQMVBBQKHGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17N3O2/c1-13-6-3-4-7-17(13)22-21-15-9-10-16(14(2)12-15)20-19(23)18-8-5-11-24-18/h3-12H,1-2H3,(H,20,23)
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| Chemical Name |
N-[2-methyl-4-[(2-methylphenyl)diazenyl]phenyl]furan-2-carboxamide
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| Synonyms |
CHD5; CHD 5; CHD-5
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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 | 3.1313 mL | 15.6563 mL | 31.3126 mL | |
| 5 mM | 0.6263 mL | 3.1313 mL | 6.2625 mL | |
| 10 mM | 0.3131 mL | 1.5656 mL | 3.1313 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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