| PDM 2potent and selective aryl hydrocarbon receptor (AhR) antagonist |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 688348-25-6 | SDF | Download SDF |
| Chemical Name | 1,3-dichloro-5-[(1E)-2-(4-chlorophenyl)ethenyl]-benzene | ||
| Canonical SMILES | Clc1ccc(cc1)C=C/c1cc(Cl)cc(Cl)c1 | ||
| Formula | C14H9Cl3 | M.Wt | 283.6 |
| Solubility | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Ki = 1.2 nM
PDM 2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
The aryl hydrocarbon receptor (AhR) is a ligand-dependent intracellular transcription factor whose ligands include some of the most infamous xenobiotics, such as dioxin, benzo[a]pyrene, and various polyaromatics from soot and coal tar.
In vitro: In a previous screening study, it was found that the replacement of resveratrol hydroxyls by the same substituent produced compounds with the following order of affinity: OH (resveratrol) , OMe < f="">< cf3="">< cl="" (pdm="" 2).="" pdm="" 2="" exhibited="" a="" ki="" of="" 1.25="" for="" ahr="" and="" no="" affinity="" for="" er,="" indicating="" that="" replacement="" of="" hydroxyl="" with="" chloride="" could="" abolish="" binding="" on="" er="" and="" dramatically="" increase="" the="" affinity="" for="" ahr.="" moreover,="" among="" its="" analogs="" pdm="" 2="" was="" the="" most="" potent="" ahr="" antagonists="" in="" this="" series,="" being="" 10-fold="" more="" efficient="" than="" resveratrol.="" pdm="" 2,="" devoid="" of="" measurable="" affinity="" for="" er,="" did="" not="" display="" any="" effect="" on="" er-driven="" transcription.="" therefore,="" pdm="" 2="" was="" considered="" as="" a="" selective="" ahr="" modulator="" with="" regard="" to="" er.="" in="" addition,="" its="" trimethoxylated="" derivatives="" and="" 3,5-methoxy="" derivatives="" were="" able="" to="" induce="" cytotoxicity="" at="" doses="" lower="" than="" 100="" nm,="" which="" was="" consistent="" with="" previous="" data.="" 3,5-methoxy="" derivatives,="" however,="" only="" showed="" cytotoxicity="" at="" concentrations="" higher="" than="" 10="" μm="">
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:[1] de Medina, P.,Casper, R.,Savouret, J.F., et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. Journal of Medicinal Chemistry 48, 287-291 (2005).
