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Submit ReviewRaloxifene hydrochloride is a selective estrogen receptor modulator (SERM) that binds to ERα and ERβ, and tissue-dependently activates or blocks estrogen-induced transcription. Acts as an antiestrogen in breast and uterine tissue, but displays estrogen agonist activity in bone. In D12 rat hypothalamic cells, inhibits progesterone receptor induction by estrogen with an IC50 of 1 nM.
Raloxifene hydrochloride 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 | 510.04 |
公式 | C28H27NO4S.HCl |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 82640-04-8 |
PubChem ID | 54900 |
InChI Key | BKXVVCILCIUCLG-UHFFFAOYSA-N |
Smiles | Cl.OC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(OCCN3CCCCC3)C=C2)C2=CC=C(O)C=C2S1 |
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 | |||
DMSO | 25.5 | 50 |
以下数据基于产品分子量 510.04。 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 |
---|---|---|---|
0.5 mM | 3.92 mL | 19.61 mL | 39.21 mL |
2.5 mM | 0.78 mL | 3.92 mL | 7.84 mL |
5 mM | 0.39 mL | 1.96 mL | 3.92 mL |
25 mM | 0.08 mL | 0.39 mL | 0.78 mL |
参考文献是支持产品生物活性的出版物。
Fitzpatrick et al (1999) Effect of estrogen agonists and antagonists on induction of progesterone receptor in a rat hypothalamic cell line. Endocrinology 140 3928 PMID: 10465261
Bryant (2001) Mechanism of action and preclinical profile of raloxifene, a selective estrogen receptor modulator. Rev.Endocr.Metab.Disord. 2 129 PMID: 11704975
Hibner et al (2004) Effects of ralox. hydrochloride on endometrial cancer cells in vitro. Gynecologic Oncol. 93 642
Todorova (2011) Tamoxifen and ralox. suppress the proliferation of estrogen receptor-negative cells through inhibition of glutamine uptake. Cancer Chemother. Pharmacol. 67 285 PMID: 20383709
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关键词: Raloxifene hydrochloride, Raloxifene hydrochloride supplier, Selective, estrogen, receptor, modulators, SERM, ER, Estrogen, Receptors, LY139481, amino, acid, transporter, 2, ASCT2, LY, 139481, Keoxifene, and, Related, 2280, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Raloxifene hydrochloride 的部分引用包括:
Nicholson et al (2015) Estrogen receptor-α is a key mediator and therapeutic target for bladder complications of benign prostatic hyperplasia. Am J Physiol Heart Circ Physiol 193 722 PMID: 25167991
Morikawa et al (2022) Pharmacological characterization of AS2690168, a novel small molecule RANKL signal transduction inhibitor. Eur.J.Pharmacol. 924 174941 PMID: 35398031
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