Catalog Number: 2280
Alternate Names: LY 139481, Keoxifene
Chemical Name: [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-methanone hydrochloride
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.
Technical Data
  • M.Wt:
    510.04
  • Formula:
    C28H27NO4S.HCl
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    82640-04-8
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.
Background References
  1. Effect of estrogen agonists and antagonists on induction of progesterone receptor in a rat hypothalamic cell line.
    Fitzpatrick et al.
    Endocrinology, 1999;140:3928
  2. Mechanism of action and preclinical profile of raloxifene, a selective estrogen receptor modulator.
    Bryant
    Rev.Endocr.Metab.Disord., 2001;2:129
  3. Effects of raloxifene hydrochloride on endometrial cancer cells in vitro.
    Hibner et al.
    Gynecologic Oncol., 2004;93:642
  4. Tamoxifen and raloxifene suppress the proliferation of estrogen receptor-negative cells through inhibition of glutamine uptake.
    Todorova et al.
    Cancer Chemother. Pharmacol., 2011;67:285
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Raloxifene hydrochloride include:

1 Citations: Showing 1 - 1

  1. Estrogen receptor-α is a key mediator and therapeutic target for bladder complications of benign prostatic hyperplasia.
    Authors: Nicholson Et al.
    Am J Physiol Heart Circ Physiol 2015;193:722

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