产品名称
4-Hydroxytamoxifen Ready Made Solution, 5 mg/mL in ethanol: isopropanol (95:5)
生物来源
synthetic
质量水平
表单
solution
浓度
5 mg/mL in ethanol: isopropanol (95:5)
运输
dry ice
储存温度
−20°C
SMILES字符串
N(CCOc1ccc(cc1)\C(=C(\CC)/c3ccccc3)\c2ccc(cc2)O)(C)C
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
相关类别
生化/生理作用
4-羟基他莫昔芬是他莫昔芬的活性代谢产物。
4-羟基他莫昔芬是他莫昔芬的活性代谢产物。4-羟基他莫昔芬在人肝脏中由细胞色素 P450 2D6 形成，是一种强效选择性雌激素受体拮抗剂。4-羟基他莫昔芬用于刺激 LC3 脂化，并以超氧化物依赖的方式形成自噬囊泡。在原代培养的人肝细胞中，他莫昔芬和 4-羟基他莫昔芬显著诱导细胞色素 P450 3A4（一种主要的药物代谢酶）。4-羟基他莫昔芬经历反 (E-Z) 异构化—这一过程发生在所有常见的实验室溶剂中。
4-羟基他莫昔芬的反式 异构体具有抗雌激素活性，而 顺式 4-羟基他莫昔芬是雌激素受体的关键激动剂。4-羟基他莫昔芬通过激活 乳腺癌细胞中p38 通路促进凋亡。
制备说明
4-羟基他莫昔芬为 13 mM 溶液。推荐工作浓度为 10-100μM。因此，4-羟基他莫昔芬制备液应在细胞培养基中以 1:130-1:1,300 稀释。
警示用语：
Danger
危险分类
Aquatic Chronic 3 - Carc. 1B - Eye Irrit. 2 - Flam. Liq. 2 - Repr. 1B
储存分类代码
3 - Flammable liquids
WGK
WGK 3
闪点(°F)
55.4 °F
闪点(°C)
13 °C
法规信息
危险化学品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Characterization of tamoxifen and 4-hydroxytamoxifen glucuronidation by human UGT1A4 variants.
Sun D, et al.
Breast Cancer Research, 8(4), R50-R50 (2006)
Activation of the p38 mitogen-activated protein kinase pathway by estrogen or by 4-hydroxytamoxifen is coupled to estrogen receptor-induced apoptosis.
Zhang C C and Shapiro D J
The Journal of Biological Chemistry, 275(1), 479-486 (2000)
Izumi Kaji et al.
Gastroenterology, 159(4), 1390-1405 (2020-06-15)
Myosin VB (MYO5B) is an essential trafficking protein for membrane recycling in gastrointestinal epithelial cells. The inactivating mutations of MYO5B cause the congenital diarrheal disease, microvillus inclusion disease (MVID). MYO5B deficiency in mice causes mislocalization of SGLT1 and NHE3, but
Kindlin-2 preserves integrity of the articular cartilage to protect against osteoarthritis.
Wu, et al.
Nature aging, 2, 332-347 (2023)
Izumi Kaji et al.
JCI insight, 6(16) (2021-07-02)
Functional loss of myosin Vb (MYO5B) induces a variety of deficits in intestinal epithelial cell function and causes a congenital diarrheal disorder, microvillus inclusion disease (MVID). The impact of MYO5B loss on differentiated cell lineage choice has not been investigated.
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