research use only

Raloxifene HCl Estrogen/progestogen Receptor modulator

Name: Raloxifene HCl
Brand: Selleck Chemicals
SKU: S1227
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S1227

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.

Chemical Structure

Molecular Weight: 510.04

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Opioid Receptor THR PGES Aromatase 5-alpha Reductase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
Related Products	Cholesterol Endoxifen HCl G15 Licochalcone A AZD9496 PHTPP Liquiritigenin Brilanestrant (GDC-0810) Pregnenolone Estriol Lasofoxifene Tartrate Equol Genistin (Genistoside) Erteberel (LY500307) Elacestrant (RAD1901) Dihydrochloride GSK5182

Chemical Information, Storage & Stability

Molecular Weight	510.04	Formula	C₂₈H₂₇NO₄S.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	82640-04-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY156758 (Keoxifene) HCl			Smiles	C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	1% methylcellulose Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (19.61mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 1% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Features	Raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk.
Targets/IC₅₀/Ki	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]
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]
References	https://pubmed.ncbi.nlm.nih.gov/14709625/ https://pubmed.ncbi.nlm.nih.gov/8612550/ https://pubmed.ncbi.nlm.nih.gov/8282823/ https://pubmed.ncbi.nlm.nih.gov/8156931/ https://pubmed.ncbi.nlm.nih.gov/8666168/ https://pubmed.ncbi.nlm.nih.gov/10963646/

Applications

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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	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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):