2,3',4,5'-四甲氧基二苯乙烯

2,3',4,5'-四甲氧基二苯乙烯化学性质

熔点 :78-79 °C
沸点 :459.9±40.0 °C(Predicted)
密度 :1.117±0.06 g/cm3(Predicted)
储存条件 :Sealed in dry,Store in freezer, under -20°C
溶解度 :DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:1): 500 μg/ml; DMSO: 20 mg/ml; Ethanol: 400 μg/ml
形态 :Powder
颜色 :Light yellow to yellow

2,3',4,5'-四甲氧基二苯乙烯性质、用途与生产工艺

生物活性 TMS ((E)-2,3',4,5'-tetramethoxystilbene) 是一种选择性和竞争性 CYP1B1 抑制剂，IC50 为 6 nM，Ki 值为 3 nM。TMS 对 CYP1A1 (IC50=300 nM) 和 CYP1A2 (IC50=3.1 μM) 的抑制作用较小。TMS 是白藜芦醇的甲基化衍生物，具有抗癌活性。

靶点

CYP1B1

6 nM (IC ₅₀ )

CYP1B1

3 nM (Ki)

CYP1A1

300 nM (IC ₅₀ )

CYP1A2

3.1 μM (IC ₅₀ )

体外研究

TMS, an analogue of resveratrol, is considered to be a potential cancer preventive agent since it is a potent inhibitor of CYP1B1. To assess survival of MCF-7 cells exposed to 1 μM benzo[a]pyrene (BP), 1 μM BP+1 μM TMS and 1 μM BP+4 μM TMS, cells ae incubated for up to 72 h without a media change. Luminescence units from exposed cells, expressed as a percentage of luminescence units from solvent (DMSO)-treated cells at the same time intervals. In all exposure groups, cell viability remains >90% for the first 24 h, but by 72 h, cell survival drops to 60-70%.
体内研究

To determine the contribution of CYP1B1 in development of hypertension in spontaneously hypertensive rats (SHR), the effect of TMS is examined on in SHR and WKY rats. Systolic BP steadily increases in SHR from 4 weeks of age. Starting from 8 weeks of age, daily injections of TMS reduce systolic BP in SHR to levels observed at the beginning of the experiment (207±7 vs. 129±2 mmHg). Systolic BP is not altered in WKY injected with TMS or its vehicle (129±7 vs. 127±4 mmHg) .

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