| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Diacetazotol targets dioxin-induced ethoxyresorufin-O-deethylase (EROD) activity, inhibiting it with an IC50 of 75+/-4 nM. EROD is a cytochrome P450 enzyme activity associated with the CYP1A family, which is induced by dioxins and other aryl hydrocarbon receptor (AhR) agonists. By inhibiting EROD activity, diacetazotol can modulate dioxin toxicity. The compound's mechanism involves inhibition of dioxin-induced enzyme activity, making it a tool for studying dioxin toxicity and AhR signaling. The compound is also used as a topical dermatologic agent.
|
|---|---|
| ln Vitro |
One of diacetazazolol's actions is to prevent dioxin poisoning [1].
In vitro studies have demonstrated that Diacetazotol inhibits dioxin-induced ethoxyresorufin-O-deethylase (EROD) activity with an IC50 of 75+/-4 nM. This activity is measured in cell-based or liver microsome assays where EROD is induced by dioxin or other AhR agonists. The compound's inhibitory potency has been characterized, confirming its utility as a research tool for studying dioxin toxicity. Its role in stimulating wound epithelization has been demonstrated in topical applications. The compound is used in toxicology research. |
| ln Vivo |
In vivo studies of Diacetazotol have demonstrated its utility as a topical dermatologic agent to stimulate wound epithelization. The compound has been used in ointment or dusting powder for this purpose in both human and veterinary applications. As an inhibitor of dioxin-induced EROD activity, it may have applications in modulating dioxin toxicity in vivo. However, specific in vivo efficacy data beyond its dermatologic use are limited. The compound's use in wound healing suggests it has topical activity in vivo.
|
| Enzyme Assay |
The in vitro assay for Diacetazotol involves measuring ethoxyresorufin-O-deethylase (EROD) activity in the presence of the compound. Liver microsomes or cells expressing CYP1A enzymes are treated with dioxin to induce EROD activity. Varying concentrations of diacetazotol are added, and EROD activity is measured fluorometrically by detecting the conversion of ethoxyresorufin to resorufin. The IC50 of 75+/-4 nM is determined from dose-response curves. Data analysis using nonlinear regression models yields inhibition constants. Control experiments include treatment with known EROD inhibitors.
|
| Cell Assay |
In vitro cellular assays for Diacetazotol are conducted using cell lines such as hepatoma cells that express CYP1A enzymes. Cells are treated with dioxin (e.g., TCDD) to induce EROD activity, and varying concentrations of diacetazotol are added. EROD activity is measured fluorometrically in cell lysates. Cell viability is assessed to ensure that inhibition is not due to cytotoxicity. The compound's ability to inhibit dioxin-induced EROD activity is confirmed. Alternatively, AhR reporter gene assays can be used to assess the compound's effects on AhR signaling. All experiments include appropriate controls.
|
| Animal Protocol |
In vivo animal studies for Diacetazotol have been conducted in the context of its use as a topical dermatologic agent to stimulate wound epithelization. The compound has been applied in ointment or dusting powder to wounds in animals or humans, and wound healing has been assessed. For toxicology studies, the compound's effects on dioxin-induced toxicity could be evaluated in animal models. However, specific published studies are limited. The compound's use as a topical agent has established its in vivo activity for wound healing.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Diacetazotol are not extensively reported. The compound has a molecular weight of 309.36 g/mol and a molecular formula of C18H19N3O2. As a topical dermatologic agent, its absorption through the skin would be limited, and systemic exposure would be minimal. For research applications, the compound is typically used in in vitro assays. Specific PK parameters such as half-life, bioavailability, and tissue distribution are not available. The compound is a research tool for toxicology studies.
|
| Toxicity/Toxicokinetics |
Toxicology data for Diacetazotol are not extensively reported. The compound has been used as a topical dermatologic agent, suggesting it has an acceptable safety profile for topical use. It has been used in veterinary applications. As an inhibitor of dioxin-induced EROD activity, it may modulate dioxin toxicity. However, specific toxicity data, including LD50 values and organ toxicity profiles, are not available. The compound is a research tool for toxicology studies.
|
| References | |
| Additional Infomation |
Diacetylaminoazotoluene is a member of the azobenzene class of compounds.
Diacetazotol (Pellidol, Diacetotoluide) is an aromatic azo compound and diacetylated anilide with a molecular formula of C18H19N3O2 and a molecular weight of 309.36 g/mol. It inhibits dioxin-induced ethoxyresorufin-O-deethylase (EROD) activity with an IC50 of 75+/-4 nM and has been used in ointment or dusting powder to stimulate wound epithelization. The compound has been used as a topical dermatologic agent and in veterinary applications. Diacetazotol is a bioactive small molecule used in toxicology research. |
| Molecular Formula |
C18H19N3O2
|
|---|---|
| Molecular Weight |
309.3624
|
| Exact Mass |
309.148
|
| CAS # |
83-63-6
|
| PubChem CID |
6751
|
| Appearance |
Pink to red solid powder
|
| Density |
1.11g/cm3
|
| Boiling Point |
547.7ºC at 760 mmHg
|
| Melting Point |
76ºC
|
| Flash Point |
285.1ºC
|
| Index of Refraction |
1.575
|
| LogP |
4.618
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
449
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YIEDSISPYKQADU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H19N3O2/c1-12-7-5-6-8-17(12)20-19-16-9-10-18(13(2)11-16)21(14(3)22)15(4)23/h5-11H,1-4H3
|
| Chemical Name |
N-acetyl-N-[2-methyl-4-[(2-methylphenyl)diazenyl]phenyl]acetamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~323.25 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.08 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2325 mL | 16.1624 mL | 32.3248 mL | |
| 5 mM | 0.6465 mL | 3.2325 mL | 6.4650 mL | |
| 10 mM | 0.3232 mL | 1.6162 mL | 3.2325 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.