Raloxifene hydrochlorideA SERM of ERα and ERβ

Raloxifene hydrochloride (CAS 82640-04-8)

Raloxifene hydrochloride | CAS 82640-04-8 is rated 5.0 out of 5 by 1.
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Synonym: Keoxifene; LY156758
Application: A SERM of ERα and ERβ
CAS Number: 82640-04-8
Purity: ≥98%
Molecular Weight: 510.04
Molecular Formula: C28H27NO4S•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Raloxifene hydrochloride is a selective estrogen receptor modulator (SERM), binding to ERα and ERβ. Tissue-dependently blocks or activates estrogen-induced transcription. Exhibits estrogen agonist behavior in bone but acts as an anti-estrogen in breast and uterine tissue. Raloxifene hydrochloride exhibits inhibitory effects of progesterone receptor induction by estrogen in D12 rat hypothalamic cells. Raloxifene hydrochloride is a substrate of Estrogen Receptor.


References

Fitzpatrick et al (1999) Effect of estrogen agonists and antagonists on induction of progesterone receptor in a rat hypothalamic cell line. Endocrinology 140 3928. Bryant (2001) Mechanism of action and preclinical profile of raloxifene, a selective estrogen receptor modulator. Rev.Endocr.Metab.Disord. 2 129. Hibner et al (2004) Effects of raloxifene hydrochloride on endometrial cancer cells in vitro. Gynecologic Oncol. 93 642.

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mM), methanol, and ethanol (<1 mg/ml at 25° C). Insoluble in water.
Storage :
Store at -20° C
Refractive Index :
n20D 1.65 (Predicted)
IC50 :
MCF7: IC50 = 0.2 nM (human); ER α: IC50 = 0.72 nM (human); Cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity : IC50 = 5.7 nM (human); ER β: IC50 = 43 nM (human); Plasmodium falciparum: IC50 = 2.51 µM
Ki Data :
Estrogen receptor alpha: Ki= 0.37 nM (rat); Estrogen receptor beta: Ki= 2.74 nM (rat)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
54900
Merck Index :
14: 8098
MDL Number :
MFCD01938233
SMILES :
C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl

Download SDS (MSDS)

Certificate of Analysis

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Raloxifene hydrochloride  Product Citations

See how others have used Raloxifene hydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 25811655  2015. PLoS ONE. 10: e0121316.

PMID: # 23688559  Yu, DD. et al. 2013. Bioorg. Med. Chem. 21: 4266-78.

PMID: # 23089292  2012. Eur J Pharm Sci. 47: 842-7.

Citations 1 to 3 of 3 total

Aslam alikium can u please explain me about mechanism of this inhibitors that in which manner thhis inhibitors act on estrogen

Asked by: Anam riaz
Thank you for your inquiry and your interest in this product. For further details regarding the inhibitory mechanism of Raloxifene hydrochloride (CAS 82640-04-8) please refer to the product citations and references provided on this site. Please contact Technical Service by phone, (800)-457-3801 option 2, email &lt;scbt@scbt.com&gt;, or by live chat directly on our website, www.scbt.com if you have any further questions.
Answered by: Technical Support Europe
Date published: 2017-12-28
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Rated 5 out of 5 by from Manni A; et al Manni A; et al. (PubMed ID: 26339626) Raloxifene hydrochloride, antiestrogen and proven to decrease the frequency of estrogen receptor positive tumors. -SCBT Publication Review
Date published: 2015-02-23
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