PDM 2

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PDM 2

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CAS NO:

688348-25-6

包装与价格：

包装	价格(元)
50mg	询价
100mg	询价

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	283.6
Cas No.	688348-25-6
Formula	C₁₄H₉Cl₃
Solubility	≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Name	1,3-dichloro-5-[(1E)-2-(4-chlorophenyl)ethenyl]-benzene
Canonical SMILES	Clc1ccc(cc1)\C=C/c1cc(Cl)cc(Cl)c1
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).