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Raloxifene HCl

Name: Raloxifene HCl
Brand: Selleck Chemicals
SKU: S1227
Rating: 5 (12 reviews)

Synonyms: LY156758 (Keoxifene) HCl

Catalog No.S1227 Purity: 99.99%

Raloxifene (LY156758, Keoxifene) HCl is a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

Raloxifene HCl Chemical Structure

CAS: 82640-04-8

Selleck's Raloxifene HCl has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Biological Activity

Description

Features

Raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk.

Targets

ER ^[1]
(Cell-free assay)

5.7 nM

In vitro
In vitro	Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM. ^[1] Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays. ^[2]
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	p-STAT3 / STAT3 / Survivin / Bcl-2 / Bcl-xl RhoA / Rock I / Rock II / p-MLC / MLC		28430601
	Growth inhibition assay	Cell viability		28430601

In Vivo
In vivo	Raloxifene restores both bone mineral density and TGF beta 3 messenger RNA expression in the femur to levels measured in intact rats. ^[2] Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue. ^[3] Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats. ^[4] Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats. ^[5]
Animal Research	Animal Models	ovariectomized (OVX) rat
	Dosages	10 mg/kg
	Administration	Orally

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT01973738	Unknown status	Selective Estrogen Receptor Modulator	Toshihiko Kono\|Tomidahama Hospital	January 2012	--
NCT02977949	Unknown status	Selective Estrogen Receptor Modulator (SERM)	Toshihiko Kono\|Tomidahama Hospital	January 2012	--
NCT01573637	Completed	Negative Symptoms of Schizophrenia in Post-menopausal Women.	Fundació Sant Joan de Déu\|Hospital Sant Joan de Deu\|Parc Sanitari Sant Joan de Déu\|Stanley Medical Research Institute	July 2011	Phase 3

References

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Chemical lnformation & Solubility

Molecular Weight	510.04	Formula	C₂₈H₂₇NO₄S.HCl
CAS No.	82640-04-8	SDF	Download Raloxifene HCl SDF
Smiles	C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (196.06 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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