Raloxifene (Synonyms: Keoxifene; LY156758 free base; LY139481)

Name: Raloxifene
Brand: MedChemExpress
SKU: HY-13738
Rating: 5.0 (13 reviews)

Cat. No.: HY-13738 Purity: 99.62%: Data Sheet
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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.

Raloxifene Chemical Structure

CAS No. : 84449-90-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Raloxifene:

13 Publications Citing Use of MCE Raloxifene

•Research Square Preprint. 2020 Nov 4;rs.3.rs-100914. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Estrogen receptor

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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	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]
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	10000 nM 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]
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]
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	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	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 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	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	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]
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	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	0.8 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	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	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	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	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	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	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	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	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	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]
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	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	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	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-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]
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	2000 nM 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]
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]

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

Molecular Weight

473.58

Formula

C₂₈H₂₇NO₄S

CAS No.

84449-90-1

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Purity & Documentation

Purity: 99.62%

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Data Sheet (276 KB) SDS (393 KB)

COA (255 KB) HNMR (235 KB) RP-HPLC (221 KB) MS (300 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]

Complete Stock Solution Preparation Table

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

Raloxifene Related Classifications

Cancer

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Raloxifene (Synonyms: Keoxifene; LY156758 free base; LY139481)

Customer Review

Other Forms of Raloxifene:

13 Publications Citing Use of MCE Raloxifene

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Raloxifene (Synonyms: Keoxifene; LY156758 free base; LY139481)

Customer Review

Other Forms of Raloxifene:

Raloxifene Related Antibodies

13 Publications Citing Use of MCE Raloxifene

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

Raloxifene Related Classifications

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