Raloxifene hydrochloride (Synonyms: Keoxifene hydrochloride; LY156758; LY139481 hydrochloride)

Name: Raloxifene hydrochloride
Brand: MedChemExpress
SKU: HY-13738A
Rating: 5.0 (20 reviews)

Cat. No.: HY-13738A Purity: 99.78%: Data Sheet
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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.

CAS No. : 82640-04-8

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Based on 20 publication(s) in Google Scholar

Other Forms of Raloxifene hydrochloride:

Raloxifene In-stock
Raloxifene hydrochloride (Standard) In-stock

20 Publications Citing Use of MCE Raloxifene hydrochloride

Cell Proliferation/Viability Assay

Cell Imaging/Staining

RT-PCR

: 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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: estrogen receptor^[1]

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	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]
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]
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.

Molecular Weight

510.04

Formula

C₂₈H₂₈ClNO₄S

CAS No.

82640-04-8

Appearance

Solid

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

Structure Classification

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)

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.78%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (256 KB) RP-HPLC (246 KB) LCMS (270 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]

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

Raloxifene hydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Raloxifene82640-04-8Keoxifene LY156758LY139481LY156758LY 156758LY-156758LY 139481LY-139481Estrogen Receptor/ERRAutophagyInhibitorinhibitorinhibit

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Raloxifene hydrochloride (Synonyms: Keoxifene hydrochloride; LY156758; LY139481 hydrochloride)

Customer Review

Other Forms of Raloxifene hydrochloride:

Raloxifene hydrochloride Related Antibodies

20 Publications Citing Use of MCE Raloxifene hydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

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View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Raloxifene hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Raloxifene hydrochloride Related Classifications

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