阿非昔芬
货号：
IA3930
品牌：
Jinpan
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产品简介
| MDL | MFCD00278780 |
| 别名 | 4-羟基他莫西芬，4-Hydroxytamoxifen，4-OHT |
| 英文名称 | AfiMoxifene |
| CAS | 68392-35-8 |
| 分子式 | C26H29NO2 |
| 分子量 | 387.51 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 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]。 |
| 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] |
| 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 |
| 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] |
| 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 | 5mg 10mg |
是雌激素受体 (estrogen receptor) 调节剂。