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Bazedoxifene (WAY-140424) HCl

Name: Bazedoxifene (WAY-140424) HCl
Brand: Selleck Chemicals
SKU: S2128
Rating: 5 (11 reviews)

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

For research use only.

Bazedoxifene HCl (WAY-140424, TSE-424) 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.

Bazedoxifene (WAY-140424) HCl Chemical Structure

CAS No. 198480-56-7

Selleck's Bazedoxifene (WAY-140424) HCl has been cited by 11 Publications

2 Customer Reviews

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Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway Map

Biological Activity

Description

Bazedoxifene HCl (WAY-140424, TSE-424) 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.

Targets

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]

Protocol (from reference)

Kinase Assay:^[3]	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]	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.
Animal Research:^[2]	Animal Models: Sprague Dawley rats Dosages: 0.5 and 5.0 mg/kg Administration: SC

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	507.06
Formula	C₃₀H₃₄N₂O₃.HCl
CAS No.	198480-56-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03475719	Unknown status	Drug: HUG186-B and HUG186-D\|Drug: HUG186	Osteoporosis Postmenopausal	Huons Co. Ltd.	January 11 2018	Phase 1
NCT03005340	Unknown status	Drug: Treatment B\|Drug: Treatment C\|Drug: Treatment BC	Healthy	Alvogen Korea	December 2016	Phase 1
NCT01973738	Unknown status	--	Selective Estrogen Receptor Modulator	Toshihiko Kono\|Tomidahama Hospital	January 2012	--
NCT00706225	Completed	Drug: Bazedoxifene and conjugated estrogens	Postmenopause	Wyeth is now a wholly owned subsidiary of Pfizer	June 2008	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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