| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PDM-11 targets the aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor that regulates the expression of xenobiotic-metabolizing enzymes. It acts as a high-affinity antagonist, blocking the binding of agonists to AhR. It does not activate quinone reductase, inhibit quinone reductase, or affect nitric oxide production or free radical quenching.
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| ln Vitro |
PDM-11 (tested at concentrations from 10^{-5} M to 10^{-4} M) did not significantly inhibit linoleate hydroperoxide formation in aerated micellar aqueous solutions of linoleate (10^{-2} M) under gamma irradiation (dose rate 10 Gy/min, doses up to 440 Gy). Hydroperoxide concentrations increased with radiation dose similarly to control without antioxidant (Fig. 3d). At 440 Gy, hydroperoxide concentration in presence of PDM11 was comparable to control (~258 μM). [1]
PDM-11 also did not significantly reduce conjugated diene (CD) formation. CD levels increased with radiation dose and were not significantly different from control (Fig. 5d). At 440 Gy, CD concentration in presence of PDM11 remained high (~300-350 μM), whereas resveratrol and piceatannol significantly decreased CD. [1] Radiolytic yields of hydroperoxides (G_hydro) and conjugated dienes (G_CD) for PDM-11 remained quasi-unchanged or only slowly decreased with increasing concentration (Fig. 6). At 10^{-4} M, G_hydro for PDM11 was not significantly different from control, in contrast to resveratrol (70.5% inhibition) and piceatannol (90.8% inhibition). [1] In vitro, PDM-11 is a selective, high-affinity AhR antagonist. It shows no significant protective effect against oxidation of linoleate micelles initiated by radiolysis-generated hydroxyl radicals. It does not activate quinone reductase 1, inhibit quinone reductase 2, or affect nitric oxide production or quenching of free radicals. |
| ln Vivo |
In vivo, PDM-11 has the potential to modulate AhR-mediated signaling pathways. By inhibiting AhR, it could affect the expression of AhR target genes involved in xenobiotic metabolism and immune regulation. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature.
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| Enzyme Assay |
Gamma radiolysis of water was used to generate hydroxyl radicals (•OH) and superoxide radicals (O2•-) under air. The dose rate was 10 Gy/min from a 137Cs source. Dosimetry was performed by Fricke method. At pH 10.5, in the presence of oxygen, •OH is the only initiating oxidizing species. Linoleate (10^{-2} M) was used as the lipid substrate in micellar aqueous solution (pH adjusted to 10.5 with NaOH to form sodium linoleate micelles). PDM-11 was added at concentrations ranging from 10^{-5} M to 10^{-4} M. The reaction mechanism: •OH abstracts a bis-allylic hydrogen from linoleate (LH) to form carbon-centered radical L•, which reacts with O2 to form peroxyl radical LOO•. Propagation: LOO• + LH → LOOH + L•. Termination: 2LOO• → LOOL + O2. The antioxidant effect was measured by inhibition of hydroperoxide and conjugated diene formation. [1]
Hydroperoxide analysis: Reverse-phase HPLC with chemiluminescence detection. Samples (100 μL) were mixed with methanol (400 μL), 100 μL injected. Separation on C18 (25 cm) + C8 (15 cm) columns at 40°C with methanol (94%) and 10 mM ammonium acetate pH5 (6%) as eluent. Post-column reaction: hydroperoxides react with microperoxidase (10 mg/L) and isoluminol (55 mg/L) in borate buffer (0.1 M pH9.2) (1:1 v/v) at 1.2 mL/min. Detection by luminometer. Quantification using authentic 13(S)-HPODE standard. Limit of detection: 30 pmol. [1] Conjugated diene measurement: UV-Vis absorption at 234 nm using a spectrophotometer with 0.2 cm pathlength quartz cell. The difference in absorbance between peroxidized and non-peroxidized lipid was measured. Molar extinction coefficient ε = 28,000 M^{-1} cm^{-1} was used for calculation. [1] In vitro AhR binding assays for PDM-11 are performed using cytosolic preparations from cells expressing the AhR. Radioligand binding studies employ [³H]-TCDD or other suitable tracers. Cytosolic preparations are incubated with varying concentrations of PDM-11, and bound and free ligands are separated by charcoal-dextran or filtration. IC₅₀ values are calculated from competition binding curves. |
| Cell Assay |
In vitro cell-based assays for PDM-11 are performed using cell lines that express AhR, such as HepG2 or MCF-7 cells. Cells are cultured in appropriate media and treated with PDM-11 at various concentrations prior to stimulation with an AhR agonist, such as TCDD. AhR activation is assessed by measuring the induction of CYP1A1 activity using the EROD assay. Cell viability is assessed by MTT assays.
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| Animal Protocol |
In vivo animal studies for PDM-11 would typically involve mouse models of AhR-mediated toxicity or disease. The compound is administered orally or intraperitoneally. AhR target gene expression is measured in tissues. The compound's ability to block AhR-mediated effects is assessed.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of PDM-11, such as half-life and oral bioavailability, are not extensively detailed in the available literature. It is soluble in DMSO and is typically formulated for in vivo administration. The compound is stable as a powder at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for PDM-11 are not widely available in public literature. As a research compound, it is intended for laboratory use only and is not for human therapeutic use. Standard safety precautions should be followed when handling this compound. The compound is supplied with a purity of ≥95%.
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| References |
Chem Phys Lipids.2008Sep;155(1):48-56.
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| Additional Infomation |
PDM-11 is a non-hydroxylated stilbene derivative, synthesized as a dioxine antagonist with potential affinity for arylhydrocarbon receptors (AhR) but without estrogen receptor affinity. In this study, it was used as a negative control to demonstrate that hydroxyl groups are necessary for antioxidant activity against peroxyl radicals. Unlike resveratrol and piceatannol, PDM11 (and PDM2) lack hydroxyl groups and showed no significant inhibition of linoleate peroxidation, confirming that the antioxidant mechanism involves hydrogen atom donation from hydroxyl groups to peroxyl radicals. [1]
PDM-11 is a selective, high-affinity AhR antagonist. It is a derivative of trans-resveratrol. It does not activate quinone reductase or affect nitric oxide production. This product is for research use only. |
| Molecular Formula |
C16H15CLO2
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| Molecular Weight |
274.74
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| Exact Mass |
274.076
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| CAS # |
1032508-03-4
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| Related CAS # |
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| PubChem CID |
49799318
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
409.1±35.0 °C at 760 mmHg
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| Flash Point |
155.2±21.1 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.622
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| LogP |
5.19
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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 |
19
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| Complexity |
273
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=CC(=C1)/C=C/C2=CC=C(C=C2)Cl)OC
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| InChi Key |
VPHHOTWBLKKBBT-ONEGZZNKSA-N
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| InChi Code |
InChI=1S/C16H15ClO2/c1-18-15-9-13(10-16(11-15)19-2)4-3-12-5-7-14(17)8-6-12/h3-11H,1-2H3/b4-3+
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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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 | 3.6398 mL | 18.1990 mL | 36.3980 mL | |
| 5 mM | 0.7280 mL | 3.6398 mL | 7.2796 mL | |
| 10 mM | 0.3640 mL | 1.8199 mL | 3.6398 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.
Products are for research use only; We do not sell to patients
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