4-Hydroxytamoxifen

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4-Hydroxytamoxifen

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

68392-35-8

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	387.51
Cas No.	68392-35-8
Formula	C₂₆H₂₉NO₂
Solubility	≥42 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name	4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol
Canonical SMILES	OC1=CC=C(C(C2=CC=C(OCCN(C)C)C=C2)=C(CC)C3=CC=CC=C3)C=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

作用于MCF-7和MDA-MB-231细胞增殖，IC50分别为27和18 μM。

4-Hydroxytamoxifen是一种雌激素受体调节剂。

雌激素受体可被选择性地刺激或抑制，为自身免疫疾病、前列腺和乳腺癌以及抑郁症提供有希望的治疗机会。

体外：先前进行研究以评价他莫昔芬及其活性代谢物4-hydroxytamoxifen对分离的大鼠心肌细胞机械功能和钙处理的作用。结果表明，用4-hydroxytamoxifen治疗的肌细胞对钙处理和收缩性的作用类似于他莫昔芬治疗的细胞[1]。

体内：先前的动物研究比较了用7种他莫昔芬或4-hydroxytamoxifen治疗的SD大鼠中DNA加合物形成的程度。结果表明，他莫昔芬或4-hydroxytamoxifen治疗未改变肝脏重量和微粒体率。此外，在他莫昔芬或4-hydroxytamoxifen治疗的大鼠中子宫重量显著降低，子宫过氧化物酶活性略微降低。此外，用4-hydroxytamoxifen治疗的大鼠肝DNA加合物水平与对照大鼠没有不同。同样，用他莫昔芬或4-hydroxytamoxifen治疗的大鼠子宫DNA加合物水平与对照大鼠没有不同[2]。

临床试验：先前的临床研究表明，4-hydroxytamoxifen凝胶对乳房皮肤的抗增殖作用与口服他莫昔芬相似，但对内分泌和凝血参数的作用降低[3]。

参考文献：
[1] Asp ML,Martindale JJ,Metzger JM. Direct, differential effects of tamoxifen, 4-hydroxytamoxifen, and raloxifene on cardiac myocyte contractility and calcium handling. PLoS One.2013 Oct 24;8(10):e78768.
[2] Beland FA,McDaniel LP,Marques MM. Comparison of the DNA adducts formed by tamoxifen and 4-hydroxytamoxifen in vivo. Carcinogenesis.1999 Mar;20(3):471-7.
[3] Lee O et al. A randomized phase II presurgical trial of transdermal 4-hydroxytamoxifen gel versus oral tamoxifen in women with ductal carcinoma in situ of the breast. Clin Cancer Res.2014 Jul 15;20(14):3672-82.

试验操作

Cell experiment:[1]
Cell lines	Isolated rat cardiac myocytes
Reaction Conditions	0 ~ 10 μM 4-hydroxytamoxifen
Applications	Myocytes treated with 4-hydroxytamoxifen responded similarly to tamoxifen-treated cells with regard to both contractility and calcium handling, suggesting an estrogen-receptor independent mechanism is responsible for the effects. At 10 μM, both drugs had a time-dependent effect to abolish cellular contraction.
Animal experiment:[2]
Animal models	C57BL/6 J mice, aged 6 weeks
Dosage form	6 μg/day Administered subcutaneously for 3 consecutive days
Applications	Three daily doses of 4-hydroxytamoxifen (6 μg/day) effectively attenuated methamphetamine-induced nigrostriatal dopamine depletions in both sexes of intact and gonadectomized C57BL/6 J mice. 4-OHT alone did not alter the dopamine content levels in the striatum.
Note	The technical data provided above is for reference only.
	References: 1. Asp ML, Martindale JJ, Metzger JM. Direct, differential effects of tamoxifen, 4-hydroxytamoxifen, and raloxifene on cardiac myocyte contractility and calcium handling. PLoS One, 2013, 8(10): e78768. 2. Kuo YM, Chen HH, Shieh CC, et al. 4-Hydroxytamoxifen attenuates methamphetamine-induced nigrostriatal dopaminergic toxicity in intact and gonadetomized mice. Journal of Neurochemistry, 2003, 87(6): 1436-1443.