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H7904

(Z)-4-羟三苯氧胺

≥98% (HPLC), powder, estrogen receptor modulator

别名:

4-羟基他莫昔芬, (Z)-4-(1-[4-(二甲氨基乙氧基)苯基]-2-苯基-1-丁烯基)苯酚, (Z)-4-OHT, 反式-4-羟三苯氧胺

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关于此项目

经验公式（希尔记法）:
C26H29NO2
化学文摘社编号:
68047-06-3
分子量:
387.51
UNSPSC Code:
51111800
PubChem Substance ID:
24895814
NACRES:
NA.77
MDL number:
MFCD00278780
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
300
Storage condition:
desiccated, protect from light
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产品名称

(Z)-4-羟三苯氧胺, ≥98% Z isomer

Quality Level

300

assay

≥98% (HPLC)

form

powder

storage condition

desiccated, protect from light

solubility

methanol: 10 mg/mL, ethanol: 20 mg/mL (with heating)

antibiotic activity spectrum

neoplastics

mode of action

enzyme | inhibits

originator

AstraZeneca

storage temp.

2-8°C

SMILES string

CC\C(c1ccccc1)=C(/c2ccc(O)cc2)c3ccc(OCCN(C)C)cc3

InChI

1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17,28H,4,18-19H2,1-3H3/b26-25-

InChI key

TXUZVZSFRXZGTL-QPLCGJKRSA-N

Gene Information

human ... ESR1(2099), ESR2(2100), ESRRG(2104), IL6(3569)
rat ... Ar(24208), Esr1(24890), Esr2(25149)

General description

4-羟基他莫昔芬(4-OHT)是抗雌激素药物他莫昔芬在人和其他哺乳动物中的代谢产物。Z型(反式)和E型(顺式)4-OHT异构体在未成熟大鼠中均具有抗雌激素作用。对反式的固定环(fixed ring)体系的结构-功能关系研究表明，反式异构体是一种强效抗雌激素剂，在体外T47D乳腺癌细胞中顺式异构体的抗雌激素作用相对较弱（效力低100倍）。4-OHT结合雌激素受体(ER)和雌激素相关受体(ERR)，同时具有雌激素和抗雌激素作用。这种物质是细胞渗透性的选择性雌激素受体调节剂(SERM)。与他莫昔芬和它的其他代谢物相比，4-OHT结合雌激素受体的亲和性更高，对正常人乳腺细胞和乳腺癌细胞系培养物的增殖抑制效力高50-100倍。此外，对这些细胞不添加雌激素培养、通过胰岛素或表皮生长因子诱导增殖时，4-OHT可有效抑制细胞生长。

Application

(Z)-4-羟基他莫昔芬已用于:
  • 作为培养基增补剂通过WST-1检测研究细胞活力
  • 诱导大鼠中转化生长因子-β (TGF-β基因的删除
  • 体外诱导 Cre重组酶活性

Features and Benefits

该化合物是受体分类及信号转导手册上核受体（类固醇）页面上的特色化合物。想要浏览手册的其他页面， 请单击此处。
该化合物由AstraZeneca开发。如需浏览其他药物开发的化合物和批准的药物/候选药物清单，请单击此处。

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Danger

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Carc. 1B - Repr. 1B

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type P3 (EN 143) respirator cartridges

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
128M4052V
069M4030V
13181124
049M4038V
088M4051V

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商品

CRISPR小分子增强剂

业内研究了CRISPR基因组编辑背景下的HDR调控，发现各种细胞类型中增强CRISPR介导的HDR效率的小分子。

Small Molecule CRISPR Enhancers

Modulation of homology-directed repair (HDR) within the context of CRISPR-genome editing has led to the identification of small molecules that enhance CRISPR-mediated HDR efficiency in various cell types.

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全球贸易项目编号

货号GTIN
H7904-25MG04061838446152
H7904-5MG04061833804889