| CAS |
No.68392-35-8 |
| 中文名称 |
阿非昔芬 |
| 英文名称 |
AfiMoxifene |
| 别名 |
(E/Z)-4-Hydroxytamoxifen;(E/Z)-4-羟基他莫昔芬 |
| 分子式 |
C26H29NO2 |
| 分子量 |
387.51 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00278780 |
| SMILES |
OC1=CC=C(/C(C2=CC=C(OCCN(C)C)C=C2)=C(C3=CC=CC=C3)\CC)C=C1 |
| 靶点 |
Estrogen Receptor/ERR |
| 通路 |
Endocrinology & Hormones |
| 背景说明 |
是雌激素受体 (estrogen receptor) 调节剂。 |
| 生物活性 |
4-Hydroxytamoxifen (Afimoxifene) 是tamoxifen的活性代谢产物，是一种选择性的雌激素受体调节分子，相比于tamoxifen，它对雌激素受体有更高的亲和力，在乳腺癌的治疗和化学疗法中应用广泛。[1-3] |
| In Vitro |
4-OHT具有较强的剂量和时间依赖式效应，能改变分离出来的大鼠心肌细胞的收缩功能[1]。使用4-羟他莫西芬治疗可使子宫过氧化物酶活性降低约50%[2].4-HT可激活intein-Cas9突变体的靶向修饰效率[3]。 |
| 细胞实验 |
Eight female Sprague–Dawley rats [Crl:COBS CD(SD)BR outbred，8 weeks old，obtained from the breeding colony at the National Center for Toxicological Research] were treated by gavage with seven daily doses of tamoxifen(20 mg/kg，54 μmol/kg，dissolved in 200 μl tricaprylin). Eight additional rats were treated daily for 7 days with 4-hydroxytamoxifen(21 mg/kg，54 μmol/kg，dissolved in 200 μl tricaprylin)and eight control animals were treated with 200 μl tricaprylin alone. Twenty-four hours following the last treatment，the rats were killed by exposure to carbon dioxide. Half of the animals were used to assess the induction of hepatic cytochrome P-450 and uterine peroxidase activities. The remaining rats were used to determine the DNA adducts formed in vivo[2] |
| 激酶实验 |
Uterine peroxidase activity was determined at 510 nm by oxidation of 4-aminoantipyrine in the presence of hydrogen peroxide. The hydrogen peroxide was dissolved in 50 mM Bis-Tris，1 mM EDTA，pH 7.1，instead of the recommended phosphate buffer to prevent interference in the absorbance measurements due to calcium phosphate precipitation. Hepatic microsomal ethoxyresorufin metabolism(a measure of cytochrome P-450 1A1/1A2)was determined by the procedure of Burke and co-workers. Analysis of p-nitrophenol metabolism(a measure of cytochrome P-450 2E1)was by the method of Reinke and Moyer. Determination of 4-dimethylaminoantipyrine metabolism(a measure of cytochrome P-450 3A4)was based on the procedure of Nash(40)，as modified by Cochin and Axelrod).[2] |
| 数据来源文献 |
[1] Asp ML， et al. PLoS One. 2013， 8(10):e78768.
[2] Beland FA， et al. Carcinogenesis. 1999， 20(3):471-477.
[3] Davis KM， et al. Nat Chem Biol. 2015， 11(5):316-8. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
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