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PDM 2 Sale

目录号 : GC11817

A resveratrol-based aryl hydrocarbon receptor antagonist

PDM 2 Chemical Structure

Cas No.:688348-25-6

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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 [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).

Chemical Properties

Cas No. 688348-25-6 SDF
化学名 1,3-dichloro-5-[(1E)-2-(4-chlorophenyl)ethenyl]-benzene
Canonical SMILES Clc1ccc(cc1)\C=C/c1cc(Cl)cc(Cl)c1
分子式 C14H9Cl3 分子量 283.6
溶解度 ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 3.5261 mL 17.6305 mL 35.2609 mL
5 mM 0.7052 mL 3.5261 mL 7.0522 mL
10 mM 0.3526 mL 1.763 mL 3.5261 mL
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