Raloxifene HCl

Catalog No.S1227 Synonyms: LY156758 (Keoxifene) HCl

For research use only.

Raloxifene (LY156758, Keoxifene) HCl 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 No. 82640-04-8

Selleck's Raloxifene HCl has been cited by 9 Publications

2 Customer Reviews

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Other Estrogen/progestogen Receptor Products

Biological Activity

Description Raloxifene (LY156758, Keoxifene) HCl 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.
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

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]

Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / Survivin / Bcl-2 / Bcl-xl ; RhoA / Rock I / Rock II / p-MLC / MLC 28430601 20970835
Growth inhibition assay Cell viability 28430601
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]

Protocol (from reference)

Animal Research:

[3]

  • Animal Models: ovariectomized (OVX) rat
  • Dosages: 10 mg/kg
  • Administration: Orally
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(196.06 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
1% methylcellulose
For best results, use promptly after mixing.

30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.04
Formula

C28H27NO4S.HCl

CAS No. 82640-04-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01973738 Unknown status -- Selective Estrogen Receptor Modulator Toshihiko Kono|Tomidahama Hospital January 2012 --
NCT02977949 Unknown status Drug: Raloxifene Selective Estrogen Receptor Modulator (SERM) Toshihiko Kono|Tomidahama Hospital January 2012 --
NCT01573637 Completed Drug: Raloxifene|Drug: Lactosa (placebo arm) 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Raloxifene HCl | Raloxifene HCl ic50 | Raloxifene HCl price | Raloxifene HCl cost | Raloxifene HCl solubility dmso | Raloxifene HCl purchase | Raloxifene HCl manufacturer | Raloxifene HCl research buy | Raloxifene HCl order | Raloxifene HCl mouse | Raloxifene HCl chemical structure | Raloxifene HCl mw | Raloxifene HCl molecular weight | Raloxifene HCl datasheet | Raloxifene HCl supplier | Raloxifene HCl in vitro | Raloxifene HCl cell line | Raloxifene HCl concentration | Raloxifene HCl nmr