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Raloxifene 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. Find out more about compound libraries available from Tocris.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Raloxifene hydrochloride, please let us know.
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Citations are publications that use Tocris products. Selected citations for Raloxifene hydrochloride include:
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
Do you know of a great paper that uses Raloxifene hydrochloride from Tocris? Please let us know.
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