Bazedoxifene HCl

Licensed and Manufactured by Pfizer Catalog No.S2128 Synonyms: TSE-424

Bazedoxifene HCl Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 380 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

2 Customer Reviews

  • 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.
ERα [1]
(radioligand binding assay)
ERβ [1]
(radioligand binding assay)
23 nM 89 nM
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]

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]


Kinase Assay:[3]
+ Expand

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.
Cell Research:[3]
+ Expand
  • Cell lines: MCF-7
  • Concentrations: ~10 nM
  • Incubation Time: 7 days
  • Method: For the proliferation assay, cells are plated at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1. After overnight incubation, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, cells are detached from the plate using trypsin-EDTA and counted using a Multisizer II.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Sprague Dawley rats
  • Formulation: 50% dimethylsulfoxide-50% 1× Dulbecco’s PBS
  • Dosages: 0.5 and 5.0 mg/kg
  • Administration: SC
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 101 mg/mL (199.18 mM)
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


CAS No. 198480-56-7
Storage powder
in solvent
Synonyms TSE-424

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02602704 Active not recruiting Arthritis Rheumatoid Hanyang University|Pfizer December 29 2015 Phase 4
NCT02448771 Active not recruiting Breast Cancer Stage IV|Unresectable Locally Advanced Invasive Breast Cancer|Metastatic Invasive Breast Cancer Dana-Farber Cancer Institute|Pfizer July 2015 Phase 1|Phase 2
NCT02237079 Completed Obesity|Glucose Homeostasis|Postmenopausal Symptoms Tulane University Health Sciences Center|Tulane University December 2014 Phase 4
NCT02100553 Completed Healthy Pfizer April 2014 Phase 1
NCT02090400 Completed Osteoporosis Postmenopausal Instituto Palacios|Pfizer May 2013 Phase 4
NCT01634789 Terminated Healthy Pfizer August 2012 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Estrogen/progestogen Receptor Signaling Pathway Map

Related Estrogen/progestogen Receptor Products

Tags: buy Bazedoxifene HCl | Bazedoxifene HCl ic50 | Bazedoxifene HCl price | Bazedoxifene HCl cost | Bazedoxifene HCl solubility dmso | Bazedoxifene HCl purchase | Bazedoxifene HCl manufacturer | Bazedoxifene HCl research buy | Bazedoxifene HCl order | Bazedoxifene HCl mouse | Bazedoxifene HCl chemical structure | Bazedoxifene HCl mw | Bazedoxifene HCl molecular weight | Bazedoxifene HCl datasheet | Bazedoxifene HCl supplier | Bazedoxifene HCl in vitro | Bazedoxifene HCl cell line | Bazedoxifene HCl concentration | Bazedoxifene HCl nmr
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID