4-Hydroxytamoxifen
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
| Cell experiment:[1] | |
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Cell lines |
Isolated rat cardiac myocytes |
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Reaction Conditions |
0 ~ 10 μM 4-hydroxytamoxifen |
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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] | |
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Animal models |
C57BL/6 J mice, aged 6 weeks |
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Dosage form |
6 μg/day Administered subcutaneously for 3 consecutive days |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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质量控制和MSDS
- 批次:
化学结构
