RALOXIFENE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C28H27NO4S
Molecular Weight	473.583
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC1=CC=C(C=C1)C2=C(C(=O)C3=CC=C(OCCN4CCCCC4)C=C3)C5=C(S2)C=C(O)C=C5

InChI

InChIKey=GZUITABIAKMVPG-UHFFFAOYSA-N

InChI=1S/C28H27NO4S/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29/h4-13,18,30-31H,1-3,14-17H2

HIDE SMILES / InChI

Molecular Formula	C28H27NO4S
Molecular Weight	473.583
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB00481 | https://www.drugs.com/pro/raloxifene-hydrochloride-tablets.html | https://www.ncbi.nlm.nih.gov/pubmed/11836973 | http://reference.medscape.com/drug/evista-raloxifene-342794

Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. Raloxifene binds to estrogen receptors, resulting in differential expression of multiple estrogen-regulated genes in different tissues. Raloxifene produces estrogen-like effects on bone, reducing resorption of bone and increasing bone mineral density in postmenopausal women, thus slowing the rate of bone loss. The maintenance of bone mass by raloxifene and estrogens is, in part, through the regulation of the gene-encoding transforming growth factor-β3 (TGF-β3), which is a bone matrix protein with antiosteoclastic properties. Raloxifene activates TGF-β3 through pathways that are estrogen receptor-mediated but involve DNA sequences distinct from the estrogen response element. The drug also binds to the estrogen receptor and acts as an estrogen agonist in preosteoclastic cells, which results in the inhibition of their proliferative capacity. This inhibition is thought to contribute to the drug's effect on bone resorption. Other mechanisms include the suppression of the activity of the bone-resorbing cytokine interleukin-6 promoter activity. Raloxifene also antagonizes the effects of estrogen on mammary tissue and blocks uterotrophic responses to estrogen. By competing with estrogens for the estrogen receptors in reproductive tissue, raloxifene prevents the transcriptional activation of genes containing the estrogen response element. As well, raloxifene inhibits the estradiol-dependent proliferation of MCF-7 human mammary tumor cells in vitro. The mechanism of action of raloxifene has not been fully determined, but evidence suggests that the drug's tissue-specific estrogen agonist or antagonist activity is related to the structural differences between the raloxifene-estrogen receptor complex (specifically the surface topography of AF-2) and the estrogen-estrogen receptor complex. Also, the existence of at least 2 estrogen receptors (ERα, ERβ) may contribute to the tissue specificity of raloxifene. Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. It is also used for reduction of risk and treatment of invasive breast cancer, and it also reduces breast density. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Common adverse events considered to be drug-related were hot flashes and leg cramps.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Estrogen receptor alpha 127 Target ID: CHEMBL206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18457385	Agonist 2637	22.0 nM [EC50]
Estrogen receptor beta 110 Target ID: CHEMBL242 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11906280	Agonist 2637	260.0 nM [EC50]
Estrogen receptor 71 Target ID: CHEMBL2093866 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12749898	Agonist 2637

Conditions

Condition	Modality	Highest Phase	Product
Osteoporosis in postmenopausal women 6 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Primary	Approved 8307	EVISTA Approved Use EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) Launch Date 8.816256E11
Breast cancer in postmenopausal women with osteoporosis 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Primary	Approved 8307	EVISTA Approved Use EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) Launch Date 8.816256E11
Breast cancer in postmenopausal women at high risk for invasive breast cancer 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Primary	Approved 8307	EVISTA Approved Use EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) Launch Date 8.816256E11

C_max

Value	Dose	Co-administered	Analyte	Population
0.5 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:		RALOXIFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
27.2 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:		RALOXIFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
27.7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:		RALOXIFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
180 mg 1 times / day single, oral Studied dose Dose: 180 mg, 1 times / day Route: oral Route: single Dose: 180 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Other AEs: Ataxia, Dizziness... Other AEs: Ataxia Dizziness Vomiting Rash Diarrhea Tremor Flushing Alkaline phosphatase increased Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf
600 mg 1 times / day multiple, oral Highest studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8725181/	healthy, Mean age 53.2 years n = 63 Health Status: healthy Age Group: Mean age 53.2 years Sex: F Population Size: 63 Sources: https://pubmed.ncbi.nlm.nih.gov/8725181/	Other AEs: Hot flashes... Other AEs: Hot flashes Sources: https://pubmed.ncbi.nlm.nih.gov/8725181/
60 mg 1 times / day multiple, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf	unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf	Other AEs: Deep vein thrombosis, Pulmonary embolism... Other AEs: Deep vein thrombosis Pulmonary embolism Stroke Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf
60 mg 1 times / day multiple, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf https://pubmed.ncbi.nlm.nih.gov/12450599/	unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf https://pubmed.ncbi.nlm.nih.gov/12450599/	Disc. AE: Vomiting, Nausea... AEs leading to discontinuation/dose reduction: Vomiting (0.3%) Nausea (0.6%) Oedema (0.6%) Muscle spasms (0.7%) Muscle related signs and symptoms NEC (1.6%) Headache (0.3%) Paralysis (0.1%) Hot flush (1.4%) Peripheral vascular disorder (1.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf https://pubmed.ncbi.nlm.nih.gov/12450599/
180 mg multiple, oral Studied dose Dose: 180 mg Route: oral Route: multiple Dose: 180 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Other AEs: Leg cramps, Dizziness... Other AEs: Leg cramps Dizziness Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf
1.5 g 1 times / day single, oral Studied dose Dose: 1.5 g, 1 times / day Route: oral Route: single Dose: 1.5 g, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	unhealthy Health Status: unhealthy Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1532			inhibitor 1570

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A5 73 KCNQ1/KCNE1 3	UGT1A1 417 UGT1A8 282 UGT1A9 378 UGT1A 7 UGT1A3 421 UGT1A4 345 UGT1A6 306 UGT1A7 235 UGT2B7 387 UGT2B15 202 SULT1A3 26 BCRP 545 MRP4 75

Drug as perpetrator

Target	Modality	Activity
CYP3A5 130	inhibitor 3185 Sources: https://pubs.acs.org/doi/pdf/10.1021/tx700207u Page: 1.0	yes [IC50 2.4 uM]
CYP3A4 1857	inhibitor 3185 Sources: https://pubs.acs.org/doi/pdf/10.1021/tx700207u Page: 1.0	yes [IC50 3.7 uM]
KCNQ1/KCNE1 3	inhibitor 3185 Sources: https://www.sciencedirect.com/science/article/pii/S1043661810001611 Page: 1.0	yes [IC50 4.8 uM]

Drug as victim

Target	Modality	Activity	Metabolite
UGT1A3 421	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT1A4 345	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT1A6 306	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT1A7 235	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT2B15 202	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT2B7 387	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
SULT1A3 26	substrate 3264 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes [Km 0.33 uM]
BCRP 545	substrate 3264 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-4'-Sulfate 3
BCRP 545	substrate 3264 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-6-Sulfate 3
MRP4 75	substrate 3264 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-4'-Sulfate 3
MRP4 75	substrate 3264 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-6-Sulfate 3
UGT1A 7	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes
UGT1A1 417	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes
UGT1A8 282	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes
UGT1A9 378	substrate 3264 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1603	inhibitor 1584 Sources: https://www.sciencedirect.com/science/article/pii/S1043661810001611 Page: 1.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:8772	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8772
ChemicalBook	CB1290431	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1290431
ZINC	ZINC000000538275	http://zinc15.docking.org/substances/ZINC000000538275
eMolecules	902386	https://www.emolecules.com/cgi-bin/more?vid=902386

PubMed

Title	Date	PubMed
An estrogen receptor basis for raloxifene action in bone.	1999 Apr-Jun	10418979
Comparative analyses of mechanistic differences among antiestrogens.	1999 Dec	10579349
The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation.	1999 Jun 16	10376571
Clinical effects of raloxifene hydrochloride in women.	1999 Mar 2	10068418
Raloxifene: a review of its use in postmenopausal osteoporosis.	2000 Aug	10983739
[Raloxifene (Celvista, Evista)].	2000 Feb	10748686
Chemoprevention of breast cancer with fenretinide.	2001	11434448
In silico discovery of novel retinoic acid receptor agonist structures.	2001	11405897
Update on endocrine aspects of breast cancer: report from the 23rd San Antonio Breast Cancer Symposium, San Antonio, Texas, USA, 6-9 December 2000.	2001	11305952
The prevention of breast cancer: an overview.	2001	11268709
Breast cancer chemoprevention: beyond tamoxifen.	2001	11250754
Transforming growth factors-beta are not good biomarkers of chemopreventive efficacy in a preclinical breast cancer model system.	2001	11250748
Chemoprevention of breast cancer.	2001	11225001
Estradiol signaling via sequestrable surface receptors.	2001 Apr	11250949
Can estrogen or selective estrogen-receptor modulators preserve cognitive function in elderly women?	2001 Apr 19	11309641
Cognitive function in postmenopausal women treated with raloxifene.	2001 Apr 19	11309635
Raloxifene for breast cancer prevention.	2001 Apr 25	11311092
Bone builders: preventing and treating osteoporosis.	2001 Aug	11481213
Familiar drugs may prevent cancer.	2001 Aug	11470927
Treatment of osteoporosis with bisphosphonates.	2001 Feb	11285996
Osteoporosis therapies for rheumatoid arthritis patients: minimizing gastrointestinal side effects.	2001 Feb	11182029
Molecular mechanism of action at estrogen receptor alpha of a new clinically relevant antiestrogen (GW7604) related to tamoxifen.	2001 Feb	11159857
[Prevention of breast cancer--what are the latest developments?].	2001 Jan	11242896
Drug information needs clarification.	2001 Jan	11212427
Estrogen and raloxifene activities on amyloid-beta-induced inflammatory reaction.	2001 Jan	11162193
[SERM-therapy in postmenopause. Protection of bone and breast].	2001 Jan 25	11219288
Estrogen, selective estrogen receptor modulation, and coronary heart disease: something or nothing.	2001 Jan 3	11136828
Paradoxical interactions among estrogen receptors, estrogens and SERMS: mutual annihilation and synergy.	2001 Jan-Mar	11384866
Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351.	2001 Jan-Mar	11384864
Raloxifene effect on frequency of surgery for pelvic floor relaxation.	2001 Jul	11430963
Rheumatology: 15. Osteoporosis.	2001 Jul 10	11468955
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.	2001 Jul 23	11459665
Tamoxifen, screening and new oestrogen receptor modulators.	2001 Jun	11476559
Oestrogenic effects of neonatal administration of raloxifene on hypothalamic-pituitary-gonadal axis in male and female rats.	2001 Jun	11373178
Chemoprevention of breast cancer. A joint guideline from the Canadian Task Force on Preventive Health Care and the Canadian Breast Cancer Initiative's Steering Committee on Clinical Practice Guidelines for the Care and Treatment of Breast Cancer.	2001 Jun 12	11450210
Indicators of lifetime estrogen exposure: effect on breast cancer incidence and interaction with raloxifene therapy in the multiple outcomes of raloxifene evaluation study participants.	2001 Jun 15	11408508
Selective estrogen receptor modulators. An aid in unraveling the links between estrogen and breast cancer.	2001 Mar	11296736
Comparative safety of bone remodeling agents with a focus on osteoporosis therapies.	2001 Mar	11269564
Managing menopause after breast cancer: balancing risks and benefits.	2001 Mar	11263852
Management of thrombosis in women with antiphospholipid syndrome.	2001 Mar	11219245
Anti-oestrogenic drugs and endometrial cancers.	2001 Mar 31	11323158
Effects of SERMs on important indicators of cardiovascular health: lipoproteins, hemostatic factors, and endothelial function.	2001 Mar-Apr	11275512
Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex.	2001 May 1	11325832
Cardiovascular effects of raloxifene hydrochloride.	2001 Spring	11314601

Patents

Sample Use Guides

In Vivo Use Guide

60 mg tablet orally once daily

Route of Administration: Oral

In Vitro Use Guide

MCF-7 cells were obtained from the ATCC and grown in Growth Medium (GM). The cells are grown to 80% confluency and trypsinized and washed to remove phenol red, then plated at 10,000 cells/well in Starve Medium (SM). After 2 days, the medium is removed from the cells and either fresh SM or SM plus Raloxifene is added (100 mL total volume). The next day the bDNA assay is started by adding Capture Hybridization Buffer to each capture well of the bDNA plate (all solutions supplied with QuantiGene kit). Subsequently, medium is removed from the 96-well plate containing cells and then the solution of lysis buffer and oligomers (designed by ProbeDesigner 1.0 for the gene of interest) is added to the 96-well plate (100 mL/well). The cell and lysis/ oligomer mixture is incubated for 15 min at 53 C and then vortexed for 1 min. The lysate is then transferred to the bDNA capture plate and mixed. The plate is then sealed and incubated at 53 C for 16 h. The next day, the plate is cooled for 10 min at room temperature and the Amplifier Reagent mixture is prepared. The wells are then washed twice with 200 mkL of Wash Solution A. Amplifier Reagent is added (50 mkL/well) and the plate is sealed again and incubated at 53 C for 30 min. The plate is then cooled for 10 min at room temperature (rt) and the Label Probe Reagent is prepared. The plate is washed twice with 200 mkL of Wash Solution A and 50 mkL/well of Label Probe Reagent is added. The plate is sealed and incubated at 53 C for 15 min. The plate is cooled for 10 min at rt and the Substrate Mixture is prepared. The plate is again washed twice with 200 mkL Wash Solution A and then twice with Wash Solution D. The Substrate Mixture is then added (50 mkL) and the plate is sealed. The plate is incubated at 37 C for 30 min and then read on the Quantiplex luminometer. Raloxifene is used as a positive control in this assay, and behaves as a full antagonist of estrogen-induced pS2 expression.

Substance Class	Chemical Created by `admin` on `Fri Dec 16 18:07:30 UTC 2022` Edited by `admin` on `Fri Dec 16 18:07:30 UTC 2022`
Record UNII	YX9162EO3I
Record Status	`Validated (UNII)`
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Name

Type

Language

RALOXIFENE

Official Name

English

EVIDEN

Brand Name

English

RALOXIFENE [HSDB]

Common Name

English

Raloxifene [WHO-DD]

Common Name

English

RAXETO

Brand Name

English

NSC-747974

Code

English

LY-139481

Code

English

RALOXIFENE [VANDF]

Common Name

English

RALOXIFENE [MI]

Common Name

English

RALOXIPHENE

Common Name

English

raloxifene [INN]

Common Name

English

J22.982B

Code

English

KEOXIFENE

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175826