Information
Bazedoxifene HCl (WAY-140424, TSE-424) is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to bothERαandERβwithIC50of 23 nM and 89 nM, respectively.
Targets
ERα (radioligand binding assay); ERβ (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. Bazedoxifene does not stimulate proliferation of MCF-7 cells but did inhibit 17β-estradiol-induced proliferation with IC50 of 0.19 nM.
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.
Cell Research(from reference)
Cell lines：MCF-7
Concentrations：~10 nM
Incubation Time：7 days
| Pubchem Sid | 504765115 |
|---|---|
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504765115 |
| Sonrisas canónicas | CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.Cl |
| IUPAC Name | 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol;hydrochloride |
| InChIKey | COOWZQXURKSOKE-UHFFFAOYSA-N |
| INCHI | 1S/C30H34N2O3.ClH/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31;/h6-15,20,33-34H,2-5,16-19,21H2,1H3;1H |
| Isómeros SMILES | CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.Cl |
| Peso molecular | 507.06 |
| Reaxy-Rn | 11737994 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11737994&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Clase | Indoles and derivatives |
| Subclass | Indoles |
| Intermediate Tree Nodes | Not available |
| Direct Parent | 2-phenylindoles |
| Alternative Parents | Phenylpyrroles N-alkylindoles Hydroxyindoles 3-methylindoles Phenoxy compounds Phenol ethers Azepanes Alkyl aryl ethers 1-hydroxy-2-unsubstituted benzenoids Heteroaromatic compounds Trialkylamines Azacyclic compounds Organopnictogen compounds Hydrochlorides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | 2-phenylindole - 2-phenylpyrrole - 3-alkylindole - Hydroxyindole - N-alkylindole - 3-methylindole - Phenoxy compound - Phenol ether - 1-hydroxy-2-unsubstituted benzenoid - Azepane - Alkyl aryl ether - Phenol - Monocyclic benzene moiety - Benzenoid - Substituted pyrrole - Heteroaromatic compound - Pyrrole - Tertiary aliphatic amine - Tertiary amine - Azacycle - Ether - Organic oxygen compound - Organic nitrogen compound - Organooxygen compound - Organonitrogen compound - Hydrochloride - Hydrocarbon derivative - Amine - Organopnictogen compound - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as 2-phenylindoles. These are indoles substituted at the 2-position with a phenyl group. |
| External Descriptors | Not available |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Fecha | Articulo |
|---|---|---|---|
 L2208510 | Certificate of Analysis | Jun 09, 2026 | B412101 |
| L2208511 | Certificate of Analysis | Jun 09, 2026 | B412101 |
| L2208512 | Certificate of Analysis | Jun 09, 2026 | B412101 |
| L2208513 | Certificate of Analysis | Jun 09, 2026 | B412101 |
| L2208514 | Certificate of Analysis | Jun 09, 2026 | B412101 |
| L2419230 | Certificate of Analysis | Dec 31, 2024 | B412101 |
| Solubilidad | Solubility (25°C) In vitro DMSO: 90 mg/mL (177.49 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| Peso molecular | 507.100 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 7 |
| Exact Mass | 506.234 Da |
| Monoisotopic Mass | 506.234 Da |
| Topological Polar Surface Area | 57.900 Ų |
| Heavy Atom Count | 36 |
| Formal Charge | 0 |
| Complexity | 623.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 2 |
