Bazedoxifene HCl
Licensed and Manufactured by Pfizer Catalog No.S2128 Synonyms: TSE-424
Molecular Weight(MW): 507.06
Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.
Cited by 3 Publications
2 Customer Reviews
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J Med Chem 2014 57(3), 632-41. Bazedoxifene HCl purchased from Selleck.
Effect of EC312 and BZD on the expression of ER, Cyclin D1 and phosphorylation of MAPK and AKT. T47D cells grown in 60-mm culture dishes in phenol red-free RPMI medium containing 5%DCC-FBS and treated with E2 (1nM) alone or in combination with EC312 or BZD (100nM) for 24 hours before preparation of cell lysate and analysis by western blot and quantification normalized by beta-actin.
PLoS One, 2016, 24;11(3):e0151182. Bazedoxifene HCl purchased from Selleck.
Purity & Quality Control
Choose Selective Estrogen/progestogen Receptor Inhibitors
Biological Activity
| Description | Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively. | ||||
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| In vitro |
Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene does not stimulate ERα mediated transcriptional activity and acts as an antagonist to estradiol in cultured breast cancer (bMCF-7) cells. Similar results are seen in other cell lines including CHO (ovarian), HepG2 (hepatic) or GTI-7 (neuronal) with bazedoxifene having no ERα agonist activity and acting as an antagonist to estradiol action.[2] Bazedoxifene does not stimulate proliferation of MCF-7 cells but did inhibit 17β-estradiol-induced proliferation with IC50 of 0.19 nM. [3] |
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| In vivo | In an immature rat model, bazedoxifene increases uterine wet weight 35% at a dose of 0.5 mg/kg compared to an 85% increase with raloxifene at the same dose and a 300% increase in uterine weight with ethinyl estradiol at a dose of 10 μg/kg. Ovarectomized rats treated with 0.3 mg/d bazedoxifene displayed maintenance of bone mass and bone strength similar to effects seen with 2 μg/d ethinyl estradiol, 3 mg/d raloxifene, or sham operated animals. [2] |
Protocol
| Kinase Assay:[3] |
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Ligand binding competition experiments: Test compounds are initially solubilized in DMSO and the final concentration of DMSO in the binding assay is ≤ 1%. Eight dilutions of each test compound are used as an unlabelled competitor for [3H]17β-estradiol. Typically, a set of compound dilutions would be tested simultaneously on human, rat and mouse ER-α and ER-β. The results are plotted as measured DPM vs. concentration of test compound. For dose-response curve fitting, a four parameter logistic model on the transformed, weighted data are fit and the IC50 is defined as the concentration of compound decreasing maximum [3H]estradiol binding by 50%. For active compounds, the IC50 is determined at least three times. It should be noted that IC50 values are not direct measures of a ligand’s affinity for the receptor. Rather, they can only be compared as relative values, in this case to 17β-estradiol. |
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| Cell Research:[3] |
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| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 101 mg/mL (199.18 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 507.06 |
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| Formula | C30H34N2O3.HCl |
| CAS No. | 198480-56-7 |
| Storage | powder |
| in solvent | |
| Synonyms | TSE-424 |
Bio Calculators
Molarity Calculator
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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03740009 | Recruiting | Perimenopausal Disorder|Depression | University of North Carolina Chapel Hill|Foundation of Hope North Carolina | January 2 2019 | Phase 4 |
| NCT03740009 | Recruiting | Perimenopausal Disorder|Depression | University of North Carolina Chapel Hill|Foundation of Hope North Carolina | January 2 2019 | Phase 4 |
| NCT03382314 | Completed | Osteoporosis | Hyundai Pharmaceutical Co. LTD. | October 16 2017 | Phase 1 |
| NCT03382314 | Completed | Osteoporosis | Hyundai Pharmaceutical Co. LTD. | October 16 2017 | Phase 1 |
| NCT03321318 | Active not recruiting | Healthy | Alvogen Korea | July 13 2017 | Phase 1 |
| NCT03321318 | Active not recruiting | Healthy | Alvogen Korea | July 13 2017 | Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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