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Submit ReviewTamoxifen citrate is an estrogen receptor antagonist/partial agonist. Selective and potent inhibitor of mammalian sterol isomerase. Neuroprotective in female rats in vivo. Also high affinity agonist at the membrane estrogen receptor GPER. Tamoxifen (Cat. No. 6432) is also available.
Sold with the permission of AstraZeneca UK Ltd.
Tamoxifen citrate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 563.65 |
公式 | C26H29NO.C6H8O7 |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 54965-24-1 |
PubChem ID | 2733525 |
InChI Key | FQZYTYWMLGAPFJ-OQKDUQJOSA-N |
Smiles | CC/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)/C1=CC=C(OCCN(C)C)C=C1.O=C(O)CC(O)(C(O)=O)CC(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 2.82 | 5 温和加热 | |
DMSO | 56.37 | 100 |
以下数据基于产品分子量 563.65。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.77 mL | 8.87 mL | 17.74 mL |
5 mM | 0.35 mL | 1.77 mL | 3.55 mL |
10 mM | 0.18 mL | 0.89 mL | 1.77 mL |
50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
参考文献是支持产品生物活性的出版物。
Wakeling et al (1984) Non-steroidal anti-estrogens - receptor binding and biological response in rat uterus, rat mammary carcinoma and human breast cancer cells. J.Steroid.Biochem. 20 111 PMID: 6538611
Mehta et al (2003) Tamoxifen, a selective estrogen receptor modulator, reduces ischemic damage caused by middle cerebral artery occlusion in the ovariectomized female rat. Neuroendocrinology 77 44 PMID: 12624540
Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology 146 624 PMID: 15539556
Merck Index 12 9216
Paul et al (1998) Both the immunosuppressant SR31747 and the antioestrogen tamox. bind to an emopamil-insensitive site of mammalian Δ8-Δ7 sterol isomerase. J.Pharmacol.Exp.Ther. 285 1302 PMID: 9618436
Todorova et al (2011) Tamoxifen and ralox. suppress the proliferation of estrogen receptor-negative cells through inhibition of glutamine uptake. Cancer Chemother. Pharmacol. 67 285 PMID: 20383709
If you know of a relevant reference for Tamoxifen citrate, please let us know.
关键词: Tamoxifen citrate, Tamoxifen citrate supplier, High, affinity, GPR30, agonists, Estrogen, receptor, partial, antagonists, Receptors, ER, ERR, AstraZeneca, GPER, amino, acid, transporter, 2, ASCT2, and, Related, (GPER), 0999, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Tamoxifen citrate 的部分引用包括:
Mansouri-Attia et al (2014) Soy promotes juvenile granulosa cell tumor development in mice and in the human granulosa cell tumor-derived COV434 cell line. Biol Reprod 91 100 PMID: 25165122
Gibbs et al (2014) Role of GPR30 in mediating OE effects on acetylcholine release in the hippocampus. Horm Behav 66 339 PMID: 24928571
Gutierrez et al (2014) The anticancer agent di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT) overcomes prosurvival autophagy by two mechanisms: persistent induction of autophagosome synthesis and impairment of lysosomal integrity. J Biol Chem 289 33568 PMID: 25301941
Tremere et al (2009) OE shapes auditory processing in the adult brain by regulating inhibitory transmission and plasticity-associated gene expression. J Neurosci 29 5949 PMID: 19420261
Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. Acta Pharm Sin B 6 894 PMID: 26441850
Sheng et al (2015) DMH1 (4-[6-(4-isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline) inhibits chemotherapeutic drug-induced autophagy. J Urol 5 330 PMID: 26579463
Nicholson et al (2015) Estrogen receptor-α is a key mediator and therapeutic target for bladder complications of benign prostatic hyperplasia. PLoS One 193 722 PMID: 25167991
Todd et al (2015) Wnt16 Is Associated with Age-Related Bone Loss and Estrogen Withdrawal in Murine Bone. FEMS Immunol Med Microbiol 10 e0140260 PMID: 26451596
Ronghe et al (2016) Tamoxifen synergizes with 4-(E)-{(4-hydroxyphenylimino)-methylbenzene, 1,2-diol} and 4-(E)-{(p-tolylimino)-methylbenzene-1,2-diol}, novel azaresveratrol analogs, in inhibiting the proliferation of breast cancer cells. Oncotarget 7 51747 PMID: 27351134
Antoon et al (2012) Inhibition of p38-MAPK alters SRC coactivation and estrogen receptor phosphorylation. Cancer Biol Ther 13 1026 PMID: 22825349
Wieland et al (2006) Efficient intracellular multiplication of Legionella pneumophila in human monocytes requires functional host cell L-type calcium channels. J Neurosci 47 296 PMID: 16831218
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Tamoxifen (1 ug/mL) was used to block the effects of estradiol in endocervical epithelial cells on intermediate filament (cytokeratin 18 and vimentin) expression.