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.
All Tocris products are intended for laboratory research use only.
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.96 mL | 9.8 mL | 19.61 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.92 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 raloxifene hydrochloride on endometrial cancer cells in vitro. Gynecologic Oncol. 93 642 PMID:
Todorova (2011) Tamoxifen and raloxifene suppress the proliferation of estrogen receptor-negative cells through inhibition of glutamine uptake. Cancer Chemother. Pharmacol. 67 285 PMID: 20383709
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