Cat. No.: HY-13738

Raloxifene

(Synonyms: Keoxifene; LY156758 free base; LY139481)

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.

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

Purity: 99.62%
CAS No.: 84449-90-1
Formula: C₂₈H₂₇NO₄S
Molecular Weight:473.58

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Raloxifene Chemical Structure

CAS No.: 84449-90-1

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Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

Estrogen receptor

All Estrogen Receptor/ERR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	45.6 μM Compound: Raloxifene	Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 39149110]
Calu-1	IC₅₀	8500 nM Compound: 6	Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis	[PMID: 19136975]
Cancer cell lines	IC₅₀	0.8 nM Compound: Raloxifene	In vitro inhibition of estradiol-stimulated MCF-7 breast cancer cell proliferation In vitro inhibition of estradiol-stimulated MCF-7 breast cancer cell proliferation	[PMID: 15582421]
CV-1	IC₅₀	0.46 nM Compound: Raloxifene	Antagonist activity at human ERalpha expressed in african green monkey CV1 cells assessed as inhibition of estrogen like activity after 24 hrs by luciferase reporter gene assay Antagonist activity at human ERalpha expressed in african green monkey CV1 cells assessed as inhibition of estrogen like activity after 24 hrs by luciferase reporter gene assay	[PMID: 16499324]
DU-145	EC₅₀	>50 μM Compound: Raloxifene	Antiproliferative activity against human prostate, androgen receptor positive DU145 cells after 24 hrs by MTT assay Antiproliferative activity against human prostate, androgen receptor positive DU145 cells after 24 hrs by MTT assay	[PMID: 25198997]
Fibroblast	CC₅₀	31.8 μM Compound: Raloxifene	Cytotoxicity against human HSF cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay Cytotoxicity against human HSF cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay	[PMID: 33373820]
Fibroblast	CC₅₀	69.8 μM Compound: Raloxifene	Cytotoxicity against human HSF cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HSF cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33373820]
HEK293	IC₅₀	4 nM Compound: Raloxifene	In vivo inhibition of human ERalpha/ERbeta co-expressed in HEK 293 cells; 4/60 In vivo inhibition of human ERalpha/ERbeta co-expressed in HEK 293 cells; 4/60	[PMID: 15109649]
HEK293	IC₅₀	10 μM Compound: 6	Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis	[PMID: 19136975]
HEK293	EC₅₀	0.66 nM Compound: Raloxifene	Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay	[PMID: 30940565]
HEK293	IC₅₀	0.18 nM Compound: Raloxifene	Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay	[PMID: 30940565]
HEK-293T	IC₅₀	0.3 nM Compound: Ral	Antagonist activity at human wild type ERalpha expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay Antagonist activity at human wild type ERalpha expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay	[PMID: 20659801]
HEK-293T	IC₅₀	56 nM Compound: Ral	Antagonist activity at human ERalpha E353A mutant expressed in HEK293T cells co-expressing ERE assessed as inhibition of ES8-induced transactivation by luciferase reporter gene assay Antagonist activity at human ERalpha E353A mutant expressed in HEK293T cells co-expressing ERE assessed as inhibition of ES8-induced transactivation by luciferase reporter gene assay	[PMID: 20659801]
HEK-293T	IC₅₀	577 nM Compound: Ral	Antagonist activity at human ERbeta E305A mutant expressed in HEK293T cells co-expressing ERE assessed as inhibition of ES8-induced transactivation by luciferase reporter gene assay Antagonist activity at human ERbeta E305A mutant expressed in HEK293T cells co-expressing ERE assessed as inhibition of ES8-induced transactivation by luciferase reporter gene assay	[PMID: 20659801]
HEK-293T	IC₅₀	6.9 nM Compound: Ral	Antagonist activity at human wild type ERbeta expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay Antagonist activity at human wild type ERbeta expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay	[PMID: 20659801]
HeLa	IC₅₀	2.4 nM Compound: 7	Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay	[PMID: 15658851]
HeLa	IC₅₀	22 nM Compound: 7	Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells	[PMID: 15658851]
HeLa	IC₅₀	260 nM Compound: 7	Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells	[PMID: 15658851]
HeLa	IC₅₀	341 nM Compound: 7	Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay	[PMID: 15658851]
HepG2	EC₅₀	11.71 μM Compound: 7	Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay	[PMID: 23688559]
HT-1080	IC₅₀	34 μM Compound: Raloxifene	Cytotoxicity against human HT1080 cells after 72 hrs by MTT assay Cytotoxicity against human HT1080 cells after 72 hrs by MTT assay	[PMID: 25282270]
Ishikawa	EC₅₀	0.04 nM Compound: 2 (Raloxifene)	Stimulation of alkaline phosphatase activity in Ishikawa human endometrial adenocarcinoma cells Stimulation of alkaline phosphatase activity in Ishikawa human endometrial adenocarcinoma cells	[PMID: 11738564]
Ishikawa	IC₅₀	23 nM Compound: raloxifene	Inhibition of estrogen receptor in Ishikawa cells Inhibition of estrogen receptor in Ishikawa cells	[PMID: 16722623]
Ishikawa	IC₅₀	24 nM Compound: RAL	Antagonist activity at estrogen receptor in human Ishikawa cells assessed as 17-beta-estradiol-induced alkaline phosphatase activity after 3 days by chemiluminescence assay Antagonist activity at estrogen receptor in human Ishikawa cells assessed as 17-beta-estradiol-induced alkaline phosphatase activity after 3 days by chemiluminescence assay	[PMID: 19366247]
Ishikawa	EC₅₀	20 μM Compound: Raloxifene	Antiproliferative activity against human ER-positive Ishikawa cells after 24 hrs by MTT assay Antiproliferative activity against human ER-positive Ishikawa cells after 24 hrs by MTT assay	[PMID: 25198997]
Ishikawa	IC₅₀	24.37 μM Compound: Raloxifene	Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay	[PMID: 29587221]
Ishikawa	IC₅₀	12.39 μM Compound: Raloxifene	Antiproliferative activity against human Ishikawa cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human Ishikawa cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34022716]
Ishikawa	IC₅₀	28.43 μM Compound: Raloxifene	Antiproliferative activity against ER-positive human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against ER-positive human Ishikawa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34509864]
Ishikawa	IC₅₀	0.94 nM Compound: Ral	Antiproliferative activity against human Ishikawa cells Antiproliferative activity against human Ishikawa cells	[PMID: 34710747]
MCF7	IC₅₀	0.72 nM Compound: 2, Raloxifene	In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol	[PMID: 11356100]
MCF7	IC₅₀	4.9 nM Compound: 5	Antiproliferative activity against MCF-7 cell line Antiproliferative activity against MCF-7 cell line	[PMID: 15177442]
MCF7	IC₅₀	0.8 nM Compound: Raloxifene	In vitro antagonistic activity against MCF-7 cells was tested using proliferation assay In vitro antagonistic activity against MCF-7 cells was tested using proliferation assay	[PMID: 15225685]
MCF7	IC₅₀	0.8 nM Compound: Raloxifene	In vitro antagonistic activity against MCF-7 cells was tested using proliferation assay In vitro antagonistic activity against MCF-7 cells was tested using proliferation assay	[PMID: 15225686]
MCF7	IC₅₀	170 nM Compound: 4	Displacement of [3H]estradiol from Estrogen receptor in MCF-7 cells Displacement of [3H]estradiol from Estrogen receptor in MCF-7 cells	[PMID: 1548683]
MCF7	IC₅₀	0.8 nM Compound: 2	Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol	[PMID: 16203138]
MCF7	IC₅₀	222 nM Compound: raloxifene	Inhibition of estrogen receptor in MCF7 cells Inhibition of estrogen receptor in MCF7 cells	[PMID: 16722623]
MCF7	IC₅₀	222 nM Compound: RAL	Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine incorporation assay Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine incorporation assay	[PMID: 19366247]
MCF7	IC₅₀	0.2 nM Compound: 2	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 22405286]
MCF7	EC₅₀	23 μM Compound: Raloxifene	Antiproliferative activity against human ER-negative MCF7 cells after 24 hrs by MTT assay Antiproliferative activity against human ER-negative MCF7 cells after 24 hrs by MTT assay	[PMID: 25198997]
MCF7	IC₅₀	50 μM Compound: Raloxifene	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 25282270]
MCF7	IC₅₀	15.4 μM Compound: Raloxifene	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 27155469]
MCF7	IC₅₀	13.18 μM Compound: Raloxifene	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 29587221]
MCF7	IC₅₀	12.5 μM Compound: Raloxifene	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 30384047]
MCF7	GI₅₀	0.079 nM Compound: 1	Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis	[PMID: 30990042]
MCF7	IC₅₀	12.1 μM Compound: Raloxifene	Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33373820]
MCF7	IC₅₀	5.5 μM Compound: Raloxifene	Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay Cytotoxicity against ER and PR-positive human MCF7 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay	[PMID: 33373820]
MCF7	IC₅₀	19.94 μM Compound: Raloxifene	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34022716]
MCF7	IC₅₀	21.93 μM Compound: Raloxifene	Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34509864]
MCF7	IC₅₀	0.89 nM Compound: Ral	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 34710747]
MCF7	IC₅₀	16.8 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay	[PMID: 38911151]
MCF7	IC₅₀	21.45 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay	[PMID: 38911151]
MCF7	IC₅₀	0.2 nM Compound: Raloxifene	Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-estradiol (in vitro) Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-estradiol (in vitro)	[PMID: 9003514]
MCF7	IC₅₀	0.2 nM Compound: raloxifene	Inhibition of estrogen-stimulated MCF-7 cell proliferation Inhibition of estrogen-stimulated MCF-7 cell proliferation	[PMID: 9548817]
MDA-MB-231	EC₅₀	30 μM Compound: Raloxifene	Antiproliferative activity against human ER-positive MDA-MB-231 cells after 24 hrs by MTT assay Antiproliferative activity against human ER-positive MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 25198997]
MDA-MB-231	IC₅₀	18.5 μM Compound: Raloxifene	Antiproliferative activity against human MDA-MB-231 cells Antiproliferative activity against human MDA-MB-231 cells	[PMID: 27155469]
MDA-MB-231	IC₅₀	18.5 μM Compound: Raloxifene	Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33373820]
MDA-MB-231	IC₅₀	7 μM Compound: Raloxifene	Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay Cytotoxicity against ER-negative human MDA-MB-231 cells assessed as reduction in colony formation incubated for 7 days by crystal violet staining based assay	[PMID: 33373820]
MDA-MB-231	IC₅₀	>50 μM Compound: Raloxifene	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34022716]
MDA-MB-231	IC₅₀	92.35 nM Compound: Ral	Antiproliferative activity against human MDA-MB-231 cells Antiproliferative activity against human MDA-MB-231 cells	[PMID: 34710747]
MDA-MB-231	IC₅₀	19.1 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay	[PMID: 38911151]
MDA-MB-231	IC₅₀	22 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay	[PMID: 38911151]
MDA-MB-361	IC₅₀	22.15 μM Compound: 1	Antiproliferative activity against human MDA-MB-361 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-361 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay	[PMID: 38911151]
MDA-MB-361	IC₅₀	38.9 μM Compound: 1	Antiproliferative activity against human MDA-MB-361 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay Antiproliferative activity against human MDA-MB-361 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay	[PMID: 38911151]
MDA-MB-435S	IC₅₀	26 μM Compound: Raloxifene	Cytotoxicity against human MDA-MB-435S cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435S cells after 72 hrs by MTT assay	[PMID: 25282270]
MES-SA	IC₅₀	37 μM Compound: Raloxifene	Cytotoxicity against human MES-SA cells after 72 hrs by MTT assay Cytotoxicity against human MES-SA cells after 72 hrs by MTT assay	[PMID: 25282270]
MG-22A	IC₅₀	6.8 μM Compound: Raloxifene	Cytotoxicity against mouse MG-22A cells after 72 hrs by MTT assay Cytotoxicity against mouse MG-22A cells after 72 hrs by MTT assay	[PMID: 25282270]
MIA PaCa-2	IC₅₀	26.3 μM Compound: Raloxifene	Cytotoxicity against human MIAPaCa2 cells assessed as cell viability Cytotoxicity against human MIAPaCa2 cells assessed as cell viability	[PMID: 24456369]
MRC5	IC₅₀	>100 nM Compound: Ral	Antiproliferative activity against human MRC5 cells Antiproliferative activity against human MRC5 cells	[PMID: 34710747]
NCI-H1299	IC₅₀	45 μM Compound: Raloxifene	Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay	[PMID: 39149110]
NCI-H661	IC₅₀	44.5 μM Compound: Raloxifene	Antiproliferative activity against human NCI-H661 cells measured after 48 hrs by MTT assay Antiproliferative activity against human NCI-H661 cells measured after 48 hrs by MTT assay	[PMID: 39149110]
NIH3T3	IC₅₀	7.8 μM Compound: Raloxifene	Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 25282270]
Osteoclast	IC₅₀	2 μM Compound: Raloxifene	Inhibition of bone resorption in Rabbit osteoclast cells by Bone-pit assay Inhibition of bone resorption in Rabbit osteoclast cells by Bone-pit assay	[PMID: 12270167]
PC-3	IC₅₀	>40 μM Compound: Raloxifene	Antiproliferative activity against human PC3 cells Antiproliferative activity against human PC3 cells	[PMID: 27155469]
SUM-159-PT	IC₅₀	43.2 μM Compound: Raloxifene	Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6 Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6	[PMID: 24456369]
T47D	IC₅₀	0.7 nM Compound: Raloxifene	In vitro inhibition of transcriptional activation induced by 1 nM 17-beta estradiol in T47D cells expressing estrogen receptor alpha In vitro inhibition of transcriptional activation induced by 1 nM 17-beta estradiol in T47D cells expressing estrogen receptor alpha	[PMID: 12459017]
T47D	IC₅₀	15 nM Compound: Raloxifene	In vitro inhibition of 1 nM 17-beta-estradiol induced transcriptional activation in T47D cells expressing estrogen receptor beta In vitro inhibition of 1 nM 17-beta-estradiol induced transcriptional activation in T47D cells expressing estrogen receptor beta	[PMID: 12459017]
T47D	GI₅₀	6.89 μM Compound: 3	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 5 days by crystal violet staining based analysis Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 5 days by crystal violet staining based analysis	[PMID: 38401456]
U-251	IC₅₀	19.25 μM Compound: 1	Antiproliferative activity against human U-251 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as reduction in cell viability by measuring total mitochondrial respiration incubated for 72 hrs by MTT assay	[PMID: 38911151]
U-251	IC₅₀	23.35 μM Compound: 1	Antiproliferative activity against human U-251 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay Antiproliferative activity against human U-251 cells assessed as reduction in cell viability by measuring number of adherent cells incubated for 72 hrs by crystal violet staining based assay	[PMID: 38911151]
U2OS	IC₅₀	3.1 nM Compound: 5	Ability to inhibit release of interleukin-6 from U2OS cell lines transfected with estrogen receptor alpha Ability to inhibit release of interleukin-6 from U2OS cell lines transfected with estrogen receptor alpha	[PMID: 15177442]

In Vivo

Raloxifene (4 mg/kg; intragastrically; daily for 13 weeks) significantly prevents bone loss in ovariectomized (OVX) rats^[1].

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

Animal Model:

Female, 12-week-old, Wistar rats (OVX rats)^[1]
Dosage:

4 mg/kg
Administration:

Intragastrically; daily for 13 weeks
Result:

Significantly increased the levels of E2 in OVX rats and significantly decreased the levels of BGP.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 84449-90-1
Appearance Solid
Molecular Weight 473.58
Formula C₂₈H₂₇NO₄S
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
Synonyms

Keoxifene; LY156758 free base; LY139481
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (20)

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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 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 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 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
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 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.
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
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
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
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 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.
Cell Rep Methods

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

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

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

2026 Mar 31;4(1):e100348. PMID: 41948149
bioRxiv

2025 Sep 4.
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 : 100 mg/mL (211.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.1116 mL

10.5579 mL

21.1158 mL

5 mM

0.4223 mL

2.1116 mL

4.2232 mL

10 mM

0.2112 mL

1.0558 mL

2.1116 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. 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)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. Khovidhunkit W, et al. Clinical effects of raloxifene hydrochloride in women. Ann Intern Med. 1999;130(5):431-439. [Content Brief]

[2]. Xu H, et al. Effect of caffeine on ovariectomy-induced osteoporosis in rats. Biomed Pharmacother. 2019;112:108650. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1116 mL	10.5579 mL	21.1158 mL	52.7894 mL
	5 mM	0.4223 mL	2.1116 mL	4.2232 mL	10.5579 mL
	10 mM	0.2112 mL	1.0558 mL	2.1116 mL	5.2789 mL
	15 mM	0.1408 mL	0.7039 mL	1.4077 mL	3.5193 mL
	20 mM	0.1056 mL	0.5279 mL	1.0558 mL	2.6395 mL
	25 mM	0.0845 mL	0.4223 mL	0.8446 mL	2.1116 mL
	30 mM	0.0704 mL	0.3519 mL	0.7039 mL	1.7596 mL
	40 mM	0.0528 mL	0.2639 mL	0.5279 mL	1.3197 mL
	50 mM	0.0422 mL	0.2112 mL	0.4223 mL	1.0558 mL
	60 mM	0.0352 mL	0.1760 mL	0.3519 mL	0.8798 mL
	80 mM	0.0264 mL	0.1320 mL	0.2639 mL	0.6599 mL
	100 mM	0.0211 mL	0.1056 mL	0.2112 mL	0.5279 mL

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
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Quantity:

Raloxifene

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

Traditional Chinese Medicine Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Breast Cancer Compound Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Receptor-targeted Compound Library

FDA-Approved Traditional Chinese Medicine Active Compound Library

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MCE Bioactive Compound Library

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FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Miao Ethnicity Medicine Compound Library

Tibetan Medicine Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Mongolian Medicine Compound Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Raloxifene

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Raloxifene Related Classifications

HY-13738 Related Classifications