PDM 11

PDM 11 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

Aryl hydrocarbon receptor (AhR), a ligand-dependent intracellular transcription factor, has ligands including the most infamous xenobiotics, such as benzo[a]pyrene, dioxin, and plenty of polyaromatics.

In vitro: In a previous study, PDM 11 was found to be structurally very similar to several resveratrol analogs which acted as a potent and selective AhR antagonists and agonists. One of these compounds with fluorine in place of the 4'-chlorine of PDM11 was shown to act as a AhR antagonist with a Ki of about 3 nM. This fluorine-containing compound was found to be inactive as a ligand for the estrogen receptor at even up to 100 μM. Therefore, since AhR knockout mice have been reported to be insensitive to the carcinogenic effects of classical AhR ligands, antagonists of AhR might potentially serve as therapeutic agents for the treatment for dioxin and other aryl hydrocarbon poisonings [1].

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).