Details
Stereochemistry | ACHIRAL |
Molecular Formula | C28H27NO4S.ClH |
Molecular Weight | 510.044 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.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=BKXVVCILCIUCLG-UHFFFAOYSA-N
InChI=1S/C28H27NO4S.ClH/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;1H
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
DescriptionCurator'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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11836973
Curator's Comment: The penetration of raloxifene in blood–brain barrier protected regions is low and may render the detection of any brain effect difficult at the dosage currently used in practice
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18457385 |
22.0 nM [EC50] | ||
Target ID: CHEMBL242 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11906280 |
260.0 nM [EC50] | ||
Target ID: CHEMBL2093866 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12749898 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | EVISTA Approved UseEVISTA® 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 Date1997 |
|||
Primary | EVISTA Approved UseEVISTA® 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 Date1997 |
|||
Primary | EVISTA Approved UseEVISTA® 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 Date1997 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.5 ng/mL |
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 |
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
27.7 h |
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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
Other AEs: Ataxia, Dizziness... Other AEs: Ataxia Sources: Dizziness Vomiting Rash Diarrhea Tremor Flushing Alkaline phosphatase increased |
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: |
healthy, Mean age 53.2 years n = 63 Health Status: healthy Age Group: Mean age 53.2 years Sex: F Population Size: 63 Sources: |
Other AEs: Hot flashes... |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Other AEs: Deep vein thrombosis, Pulmonary embolism... Other AEs: Deep vein thrombosis Sources: Pulmonary embolism Stroke |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Disc. AE: Vomiting, Nausea... AEs leading to discontinuation/dose reduction: Vomiting (0.3%) Sources: 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%) |
180 mg multiple, oral Studied dose Dose: 180 mg Route: oral Route: multiple Dose: 180 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: F Sources: |
Other AEs: Leg cramps, Dizziness... Other AEs: Leg cramps Sources: Dizziness |
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: |
unhealthy Health Status: unhealthy Sex: F Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Alkaline phosphatase increased | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Ataxia | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Diarrhea | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Dizziness | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Flushing | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Rash | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Tremor | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Vomiting | 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: |
healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: |
|
Hot flashes | 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: |
healthy, Mean age 53.2 years n = 63 Health Status: healthy Age Group: Mean age 53.2 years Sex: F Population Size: 63 Sources: |
|
Deep vein thrombosis | 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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
|
Pulmonary embolism | 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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
|
Stroke | 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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
|
Paralysis | 0.1% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Headache | 0.3% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Vomiting | 0.3% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Nausea | 0.6% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Oedema | 0.6% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Muscle spasms | 0.7% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Hot flush | 1.4% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Muscle related signs and symptoms NEC | 1.6% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Peripheral vascular disorder | 1.6% Disc. AE |
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: |
unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: |
Dizziness | 180 mg multiple, oral Studied dose Dose: 180 mg Route: oral Route: multiple Dose: 180 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: F Sources: |
|
Leg cramps | 180 mg multiple, oral Studied dose Dose: 180 mg Route: oral Route: multiple Dose: 180 mg Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sex: F Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubs.acs.org/doi/pdf/10.1021/tx700207u Page: 1.0 |
yes [IC50 2.4 uM] | |||
Sources: https://pubs.acs.org/doi/pdf/10.1021/tx700207u Page: 1.0 |
yes [IC50 3.7 uM] | |||
Page: 1.0 |
yes [IC50 4.8 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Page: 1.0 |
yes [Km 0.33 uM] | |||
Page: 1.0 |
yes | |||
Page: 1.0 |
yes | |||
Page: 1.0 |
yes | |||
Page: 1.0 |
yes | |||
yes | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 1.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Raloxifene and prevention of vertebral fracture (cont'd): mainly when oestrogen is contraindicated. | 2000 Dec |
|
Initiation of osteoporosis treatment after bone mineral density testing. | 2001 |
|
Alendronate: an update of its use in osteoporosis. | 2001 |
|
Chemoprevention of breast cancer with fenretinide. | 2001 |
|
In silico discovery of novel retinoic acid receptor agonist structures. | 2001 |
|
[Modern approaches to hormone therapy of breast cancer as a reflection of pathogenesis of the disease]. | 2001 |
|
[An alternative to postmenopausal Hormone Replacement Therapy? Selective Estrogens Receptors Modulators (SERMs)]. | 2001 Apr |
|
Can estrogen or selective estrogen-receptor modulators preserve cognitive function in elderly women? | 2001 Apr 19 |
|
Cognitive function in postmenopausal women treated with raloxifene. | 2001 Apr 19 |
|
Raloxifene fails to slow cognitive decline in older women. | 2001 Apr 21 |
|
Raloxifene for breast cancer prevention. | 2001 Apr 25 |
|
[SERM--selective estrogen receptor modulators]. | 2001 Apr 9 |
|
Bone builders: preventing and treating osteoporosis. | 2001 Aug |
|
Familiar drugs may prevent cancer. | 2001 Aug |
|
Estrogen-like activity of tamoxifen and raloxifene on NMDA receptor binding and expression of its subunits in rat brain. | 2001 Aug |
|
Neuroprotective properties of 17beta-estradiol, progesterone, and raloxifene in MPTP C57Bl/6 mice. | 2001 Aug |
|
Paradoxical interactions among estrogen receptors, estrogens and SERMS: mutual annihilation and synergy. | 2001 Jan-Mar |
|
Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351. | 2001 Jan-Mar |
|
Raloxifene effect on frequency of surgery for pelvic floor relaxation. | 2001 Jul |
|
Gonadotropins at menopause: the influence of obesity, insulin resistance, and estrogens. | 2001 Jul |
|
Rheumatology: 15. Osteoporosis. | 2001 Jul 10 |
|
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor. | 2001 Jul 23 |
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Effects of raloxifene and hormone replacement therapy on markers of serum atherogenicity in healthy postmenopausal women. | 2001 Jul 25 |
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Tamoxifen and contralateral breast cancer: the other side. | 2001 Jul 4 |
|
Estradiol regulates monocyte chemotactic protein-1 in human coronary artery smooth muscle cells: a mechanism for its antiatherogenic effect. | 2001 Jul-Aug |
|
Tamoxifen, screening and new oestrogen receptor modulators. | 2001 Jun |
|
A non-calcemic analog of 1 alpha,25 dihydroxy vitamin D(3) (JKF) upregulates the induction of creatine kinase B by 17 beta estradiol in osteoblast-like ROS 17/2.8 cells and in rat diaphysis. | 2001 Jun |
|
Estrogenic and antiestrogenic effects of raloxifene on collagen metabolism in breast cancer MCF-7 cells. | 2001 Jun |
|
Medication update. | 2001 Jun |
|
NIH Consensus Development Panel on Osteoporosis Prevention, Diagnosis, and Therapy, March 7-29, 2000: highlights of the conference. | 2001 Jun |
|
Tibolone and its effects on bone: a review. | 2001 Jun |
|
Osteoporosis. | 2001 Jun |
|
Tamoxifen to raloxifene and beyond. | 2001 Jun |
|
Breast cancer chemoprevention: current status and future directions. | 2001 Jun |
|
Effects of the selective estrogen receptor modulator, raloxifene, on the somatotropic axis and insulin-glucose homeostasis. | 2001 Jun |
|
Effect of physicians opinion on patients' choice of treatment. | 2001 Jun |
|
Oestrogenic effects of neonatal administration of raloxifene on hypothalamic-pituitary-gonadal axis in male and female rats. | 2001 Jun |
|
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 |
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Anti-oestrogenic drugs and endometrial cancers. | 2001 Mar 31 |
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Prevention and treatment of osteoporosis. | 2001 Mar-Apr |
|
Effects of the selective oestrogen receptor modulator-raloxifene-on calcium and PTH secretory dynamics in women with osteoporosis. | 2001 May |
|
Differential SERM activation of the estrogen receptors (ERalpha and ERbeta) at AP-1 sites. | 2001 May |
|
Effects of postmenopausal hormone replacement therapy on lipid, lipoprotein, and apolipoprotein (a) concentrations: analysis of studies published from 1974-2000. | 2001 May |
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Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex. | 2001 May 1 |
|
Flexible alignment of small molecules. | 2001 May 10 |
|
Effect of tibolone and raloxifene on the tail temperature of oestrogen-deficient rats. | 2001 May 4 |
|
From adjuvant therapy to breast cancer prevention: BCPT and STAR. | 2001 May-Jun |
|
Estrogen receptor (ER)-alpha, but not ER-beta, mediates regulation of the insulin-like growth factor I gene by antiestrogens. | 2001 Sep 21 |
|
Cardiovascular effects of raloxifene hydrochloride. | 2001 Spring |
|
Regression to the mean: what does it mean? Using bone density results to monitor treatment of osteoporosis. | 2001 Spring |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12749898
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
Edited
Fri Dec 15 15:46:24 GMT 2023
by
admin
on
Fri Dec 15 15:46:24 GMT 2023
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Record UNII |
4F86W47BR6
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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EMA ASSESSMENT REPORTS |
EVISTA (AUTHORIZED: OSTEOPOROSIS, POSTMENOPAUSAL)
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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EMA ASSESSMENT REPORTS |
OPTRUMA (AUTHORIZED: OSTEOPOROSIS, POSTMENOPAUSAL)
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FDA ORPHAN DRUG |
309910
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EU-Orphan Drug |
EU/3/10/730
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EMA ASSESSMENT REPORTS |
RALOXIFENE TEVA (AUTHORIZED: OSTEOPOROSIS, POSTMENOPAUSAL)
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NCI_THESAURUS |
C1821
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Code System | Code | Type | Description | ||
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CHEMBL81
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PRIMARY | |||
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54900
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706725
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82640-04-8
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U-8
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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DBSALT000272
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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1598201
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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DTXSID1034181
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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SUB12568MIG
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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100000091054
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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166551
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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PRIMARY | RxNorm | ||
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m9485
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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PRIMARY | Merck Index | ||
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C1762
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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50740
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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4F86W47BR6
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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4F86W47BR6
Created by
admin on Fri Dec 15 15:46:24 GMT 2023 , Edited by admin on Fri Dec 15 15:46:24 GMT 2023
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Related Record | Type | Details | ||
---|---|---|---|---|
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PARENT -> SALT/SOLVATE | |||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
EP
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
|
||
|
SOLVATE->ANHYDROUS |
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
RALOXIFENE HYDROCHLORIDE IMPURITY B [EP] AMOUNT NOT SPECIFIED
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
RALOXIFENE HYDROCHLORIDE IMPURITY C [EP] AMOUNT NOT SPECIFIED
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |