| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Aryl hydrocarbon receptor (AhR) [1][2] Prostatic VEGF[1] Estrogenic[1]
|
|---|---|
| ln Vitro |
AhR modulator-1 (6-MCDF; 0.1-10 μM; 48-96 hours; ASPC-1 cells) treatment demonstrates dose-dependent growth inhibitory effects with growth inhibitory effects of 26, 43 and 99% at doses of 0.1, 1 and 10 μM, respectively[2].
|
| ln Vivo |
In C57BL/6-Tg(TRAMP)8247Ng/J mice, therapy with AhR modulator-1 (6-MCDF; 0–40 mg/kg; oral dose; daily; for 12 weeks) decreases the incidence of pelvic lymph node metastases. Furthermore, serum VEGF concentrations are lowered. There is no discernible decrease in the incidence or size of prostate tumors[1].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: ASPC-1 cells Tested Concentrations: 0.1 μM, 1 μM and 10 μM Incubation Duration: 48 hrs (hours), 72 hrs (hours), 96 hrs (hours) Experimental Results: demonstrated dose-dependent growth inhibitory effects. |
| Animal Protocol |
Animal/Disease Models: C57BL/6-Tg(TRAMP)8247Ng/J (TRAMP) mice (8-week -old)[1]
Doses: 0 mg/kg, 10 mg/kg, 40 mg/kg Route of Administration: Oral administration; daily; for 12 weeks Experimental Results: The frequency of pelvic lymph node metastasis was decreased 5-fold in mice fed the 40 mg/kg diet.Serum VEGF concentrations were also decreased. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
No information on dibenzofuran metabolism in mammals has been found in the existing literature. Bacteria such as Sphingomonas, Brevibacterium, Terrabacter, and Staphylococcus auricularis can degrade dibenzofuran to 2,2',3-trihydroxybiphenyl via dibenzofuran 4,4α-dioxygenase. (L952) |
| Toxicity/Toxicokinetics |
Toxicity Summary
Halogenated dibenzofurans (PCDF and PBDF) bind to the aryl hydrocarbon receptor (AhR), enhancing their ability to activate transcription in the promoter region of XREs (xenobiotic response elements). Specifically, AhR binds to PCDF, transporting it to the nucleus, where it interacts with hydrocarbon nuclear translocases (ARNTs) and XREs to increase the expression of CYP1A1 and aryl hydrocarbon hydroxylase (CYP1B1). The AhR signaling pathway also increases the conversion of arachidonic acid to prostaglandins via cyclooxygenase-2, alters the Wnt/β-catenin signaling pathway (downregulating Sox9), and changes the signaling of inflammatory cytokine receptors. The AhR signaling pathway also alters proteasomal degradation of steroid hormone receptors, changes cellular responses to UVB stress, and alters the differentiation of certain T cell subsets. AhR-mediated activation and alteration lead to weight loss, cancer, and thymic atrophy (characterized by immune and endocrine disorders), which are common toxic effects of PCDF and related toxic halogenated aromatic hydrocarbons. |
| References |
|
| Additional Infomation |
Chlorinated dibenzofurans (CDFs) are a class of chemical substances whose parent compound, dibenzofuran, has one to eight chlorine atoms attached to its carbon atoms. The CDF family comprises 135 different compounds (called homologues), each with varying health and environmental effects. Of these 135 compounds, those containing chlorine atoms at positions 2, 3, 7, and 8 of the parent dibenzofuran molecule are particularly harmful. Aside from small-scale laboratory use for research purposes, CDFs are not intentionally produced in industry. Most CDFs are produced in small quantities as impurities in products and processes that use chlorinated compounds. Only a few of these 135 CDF compounds are produced in sufficiently large quantities to allow for the study of their properties, such as color, odor, taste, and toxicity. (L952)
|
| Molecular Formula |
C13H7CL3O
|
|---|---|
| Molecular Weight |
285.55
|
| Exact Mass |
283.956
|
| CAS # |
118174-38-2
|
| PubChem CID |
114900
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
6.1
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
17
|
| Complexity |
298
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
RPMARRQIRRJWEZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H7Cl3O/c1-6-2-7(14)3-9-12-10(16)4-8(15)5-11(12)17-13(6)9/h2-5H,1H3
|
| Chemical Name |
1,3,8-trichloro-6-methyldibenzofuran
|
| 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) |
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
|
|---|---|
| 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 | 3.5020 mL | 17.5101 mL | 35.0201 mL | |
| 5 mM | 0.7004 mL | 3.5020 mL | 7.0040 mL | |
| 10 mM | 0.3502 mL | 1.7510 mL | 3.5020 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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