Raloxifene hydrochloride

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Cat.No. 2280 - Raloxifene hydrochloride | C28H27NO4S.HCl | CAS No. 82640-04-8
Description: Selective estrogen receptor modulator (SERM)
Alternative Names: LY 139481, Keoxifene
Chemical Name: [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-methanone hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature
Pathways

Biological Activity

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.

Compound Libraries

Raloxifene hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 510.04
Formula C28H27NO4S.HCl
Storage Desiccate at +4°C
Purity ≥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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.5 50

Preparing Stock Solutions

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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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1 Citation for Raloxifene hydrochloride

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


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Literature in this Area

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Cancer

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Nuclear Receptors

Nuclear Receptors Product Listing

A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:

  • Androgen Receptors
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Pathways for Raloxifene hydrochloride

Estrogen

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.