Cat. No.: HY-13738A

Raloxifene hydrochloride

(Synonyms: Keoxifene hydrochloride; LY156758; LY139481 hydrochloride)

20 Cited Publications

Customer Review

Based on 20 publication(s) in Google Scholar

Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

For research use only. We do not sell to patients.

Purity: 99.78%
CAS No.: 82640-04-8
Formula: C₂₈H₂₈ClNO₄S
Molecular Weight:510.04

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Raloxifene hydrochloride Chemical Structure

CAS No.: 82640-04-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: estrogen receptor^[1]

All Estrogen Receptor/ERR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>15 μM Compound: Raloxifene.HCl	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31382118]
HT-29	IC₅₀	>15 μM Compound: Raloxifene.HCl	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31382118]
Ishikawa	IC₅₀	10.53 μg/mL Compound: Raloxifene Hydrochloride	Inhibition of estradiol-induced proliferation in human Ishikawa cells after 72 hrs by Cell-titer-Glo assay Inhibition of estradiol-induced proliferation in human Ishikawa cells after 72 hrs by Cell-titer-Glo assay	[PMID: 28442256]
Ishikawa	IC₅₀	4.32 nM Compound: 1	Inhibitory concentration against estrogen-induced proliferation of Ishikawa uterine cells by 1 nM E2 Inhibitory concentration against estrogen-induced proliferation of Ishikawa uterine cells by 1 nM E2	[PMID: 16250633]
MCF7	EC₅₀	0.02 nM Compound: 5 (Raloxifene HCl)	Effective concentration against MCF-7 breast tumor cells using MCF-7 assay. Effective concentration against MCF-7 breast tumor cells using MCF-7 assay.	[PMID: 12825935]
MCF7	IC₅₀	>15 μM Compound: Raloxifene.HCl	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31382118]
MCF7	IC₅₀	0.2 nM Compound: Raloxifen HCl	Inhibition of 17-beta-estradiol induced MCF-7 cell proliferation Inhibition of 17-beta-estradiol induced MCF-7 cell proliferation	[PMID: 11495597]
MCF7	IC₅₀	0.37 nM Compound: 1	Half maximal inhibitory concentration against estrogen-induced proliferation of MCF-7 breast cells by 10 pM E2 Half maximal inhibitory concentration against estrogen-induced proliferation of MCF-7 breast cells by 10 pM E2	[PMID: 16250633]
MCF7	IC₅₀	0.4 nM Compound: 2 (raloxifene HCl)	Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells	[PMID: 9154963]
MCF7	IC₅₀	0.72 nM Compound: Raloxifene HCl	Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha	[PMID: 10673099]
MCF7	IC₅₀	0.98 μg/mL Compound: Raloxifene Hydrochloride	Inhibition of estradiol-induced proliferation in human MCF7 cells after 72 hrs by Cell-titer-Glo assay Inhibition of estradiol-induced proliferation in human MCF7 cells after 72 hrs by Cell-titer-Glo assay	[PMID: 28442256]
MCF7	IC₅₀	1.4 nM Compound: 5 (Raloxifene HCl)	Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay. Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay.	[PMID: 12825935]
MDA-MB-231	IC₅₀	11.21 μg/mL Compound: Raloxifene Hydrochloride	Inhibition of estradiol-induced proliferation in human MDA-MB-231 cells after 72 hrs by Cell-titer-Glo assay Inhibition of estradiol-induced proliferation in human MDA-MB-231 cells after 72 hrs by Cell-titer-Glo assay	[PMID: 28442256]

In Vitro

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^[1].
Raloxifene is a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, exhibits K_i values of 0.87 to 1.4 nM^[2].
Raloxifene is also a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a K_i value of 51 nM^[2].
Raloxifene (0-80 μM; 48 hours) significantly decreased in mouse mammary carcinoma BJMC3879luc2 cells viability as a concentration manner in BJMC3879luc2 cells^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[5]

Cell Line:

BJMC3879luc2 cells
Concentration:

0 μM, 10 μM, 20 μM, 40 μM, 80 μM
Incubation Time:

48 hours
Result:

Reduced BJMC3879luc2 cell viability.

In Vivo

Raloxifene (3 mg/kg; once daily) 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^[3].
Raloxifene (oral administration; 0.1 mg/kg-10 mg/kg; 5 weeks) increases bone mineral density in the distal femur and proximal tibia. It reduces serum cholesteroloral with ED₅₀ of 0.2 mg/kg in ovariectomized (OVX) rat^[4].
Raloxifene (subcutaneously implanted mini-osmotic pumps; 18 or 27 mg/kg; once daily; 6 weeks) significantly suppresses tumor volumes in mice, in addition, the multiplicity of lymph node metastasis is also significantly decreased^[5].
.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Syngeneic BALB/c mice with BJMC3879luc2 cells^[5]
Dosage:

18 or 27 mg/kg
Administration:

Subcutaneously implanted mini-osmotic pumps
Result:

Inhibited tumor growth in mice.

Chemical Information

CAS No. 82640-04-8
Appearance Solid
Molecular Weight 510.04
Formula C₂₈H₂₈ClNO₄S
Color Light yellow to yellow
SMILES

O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C31)C4=CC=C(OCCN5CCCCC5)C=C4.Cl
Synonyms

Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
Structure Classification
- Alkaloids
- Piperidine Alkaloids
- Phenols
- Polyphenols
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (20)

All Cell Proliferation/Viability AssayOthersCell Imaging/StainingRT-PCR

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Journal Impact Factor

Exp Mol Med

Comprehensive profiling of RNA modification-related genes identifies RNA m7G binding protein CBP20 as a therapeutic target for tumor growth inhibition. [Abstract]

2025 Sep;57(9):1978-1995. PMID: 40887503

Raloxifene hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2025 Sep;57(9):1978-1995. [Abstract]

The effect of Raloxifene, Purpurogallin or Enoxacin on cancer cell viability. Cytotoxicity for each drug measured by WST after exposing the cells to the drug for 72 h in HCT116 cells.

Raloxifene hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2025 Sep;57(9):1978-1995. [Abstract]

The colony formation of HCT116 and A549 cells treating with indicated concentrations of Raloxifene, Purpurogallin or Enoxacin for 14 days.

Raloxifene hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2025 Sep;57(9):1978-1995. [Abstract]

The effect of raloxifene, purpurogallin or enoxacin on CBP20 mRNA expression. qRT–PCR was performed for CBP20 mRNA in HCT116 and A549 cells after treating Raloxifene (15 μM), Purpurogallin ( 25 μM) or Enoxacin (80 μM) for indicated time points.
Phytomedicine

Celosiae Semen and Celosin I alleviate postmenopausal osteoporosis by inhibiting ferroptosis through the Nrf2/GPX4 pathway. [Abstract]

2026 May:154:158032. PMID: 41795294
eGastroenterology

Phosphoinositide kinase PIKfyve inhibitor apilimod blocks hepatitis E virus infection. [Abstract]

2026 Mar 31;4(1):e100348. PMID: 41948149
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Free Radic Biol Med

Nuclear protein HMGN2 attenuates pyocyanin-induced oxidative stress via Nrf2 signaling and inhibits Pseudomonas aeruginosa internalization in A549 cells. [Abstract]

2017 Jul:108:404-417. PMID: 28408162

Raloxifene hydrochloride purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2017 Jul:108:404-417. [Abstract]

Intracellular ROS production stimulated by 3-h incubation of 48 and 72-h PAO1/A549 co-culture supernatants with (PAO1+Ral) or without (PAO1)100 μg/ml of raloxifene monitored by flow cytometry.
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Ecotoxicol Environ Saf

Unveiling the ESR1 dysfunction orchestrates the link per- and polyfluoroalkyl substances exposure to osteoarthritis: Insights from multi-scale evidence. [Abstract]

2025 Dec 9:309:119538. PMID: 41371105
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Int Immunopharmacol

Screening of orthopedic medicines identifies raloxifene hydrochloride as a novel ferroptosis inhibitor for spinal cord injury therapy. [Abstract]

2024 Nov 6;143(Pt 3):113542. PMID: 39510030

Raloxifene hydrochloride purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2024 Nov 6;143(Pt 3):113542. [Abstract]

Raloxifene hydrochloride (1 μM). CCK8 assay was used to screen drugs by measuring cell viability of PC12 cells.
Mol Neurobiol

Raloxifene Prevents Chemically-Induced Ferroptotic Neuronal Death In Vitro and In Vivo. [Abstract]

2025 Mar;62(3):3934-3955. PMID: 39354232
ACS Omega

Discovery of PLpro and Mpro Inhibitors for SARS-CoV-2. [Abstract]

2023 Jun 14;8(25):22603-22612. PMID: 37387790
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569
Med Sci Monit

Estrogen Modulates Cartilage and Subchondral Bone Remodeling in an Ovariectomized Rat Model of Postmenopausal Osteoarthritis. [Abstract]

2019 Apr 29:25:3146-3153. PMID: 31031401
Hematology

Raloxifene inhibits the proliferation of pediatric acute myeloid leukemia by targeting the ANP32B gene and regulating C-MYC expression. [Abstract]

2026 Dec 31;31(1):2691533. PMID: 42372253
bioRxiv

2025 Sep 4.
Biomed Pharmacother

Identification of the atypical antipsychotic Asenapine as a direct survivin inhibitor with anticancer properties and sensitizing effects to conventional therapies. [Abstract]

2025 Jan:182:117756. PMID: 39693907
Eberhard Karls Universität Tübingen

2021 Aug.
Res Sq

Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]

2020 Dec 31:rs.3.rs-100914. PMID: 33173861

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (65.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9606 mL

9.8032 mL

19.6063 mL

5 mM

0.3921 mL

1.9606 mL

3.9213 mL

10 mM

0.1961 mL

0.9803 mL

1.9606 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yang, N.N., et al., Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology, 1996. 137(5): p. 2075-84. [Content Brief]

[2]. Obach, R.S., Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos, 2004. 32(1): p. 89-97. [Content Brief]

[3]. Sato, M., M.K. Rippy, and H.U. Bryant, Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J, 1996. 10(8): p. 905-12. [Content Brief]

[4]. Black, L.J., et al., Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest, 1994. 93(1): p. 63-9. [Content Brief]

[5]. Shibata MA, et al. Raloxifene inhibits tumor growth and lymph node metastasis in a xenograft model of metastatic mammary cancer.BMC Cancer. 2010 Oct 19;10:566. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9606 mL	9.8032 mL	19.6063 mL	49.0158 mL
	5 mM	0.3921 mL	1.9606 mL	3.9213 mL	9.8032 mL
	10 mM	0.1961 mL	0.9803 mL	1.9606 mL	4.9016 mL
	15 mM	0.1307 mL	0.6535 mL	1.3071 mL	3.2677 mL
	20 mM	0.0980 mL	0.4902 mL	0.9803 mL	2.4508 mL
	25 mM	0.0784 mL	0.3921 mL	0.7843 mL	1.9606 mL
	30 mM	0.0654 mL	0.3268 mL	0.6535 mL	1.6339 mL
	40 mM	0.0490 mL	0.2451 mL	0.4902 mL	1.2254 mL
	50 mM	0.0392 mL	0.1961 mL	0.3921 mL	0.9803 mL
	60 mM	0.0327 mL	0.1634 mL	0.3268 mL	0.8169 mL

Keywords

Raloxifene hydrochloride

20 Cited Publications

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Raloxifene hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Raloxifene hydrochloride

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Raloxifene hydrochloride Related Classifications

HY-13738A Related Classifications