Bazedoxifene hydrochloride
Based on 19 publication(s) in Google Scholar
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 198480-56-7
- 分子式: C30H35ClN2O3
- 分子量:507.06
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
Other In-stock Forms of Bazedoxifene hydrochloride
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生物活性
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化学情報
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- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Bazedoxifene hydrochloride
More- Nat Commun. 2026 Apr 1;17(1):4716. [Abstract]
- Free Radic Biol Med. 2023 Aug 20:205:163-174. [Abstract]
- J Med Chem. 2020 Oct 8;63(19):11085-11099. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Eur J Pharmacol. 2026 Jul 15:1030:179133.
- Eur J Pharmacol. 2023 May 15:947:175681. [Abstract]
- Glia. 2023 Feb;71(2):284-304. [Abstract]
- Sci Rep. 2026 Mar 17. [Abstract]
- iScience. 2026 Feb 6;29(3):114931. [Abstract]
- Gynecol Oncol. 2019 Jul;154(1):199-206. [Abstract]
- mSphere. 2020 Apr 8;5(2):e00124-20. [Abstract]
- Arch Biochem Biophys. 2025 Jun:768:110366. [Abstract]
- Breast Cancer Res Treat. 2020 Jan;179(1):67-77. [Abstract]
- J Cell Biochem. 2023 Sep;124(9):1404-1422. [Abstract]
- Res Sq. 2026 Jul 2.
- University of Colorado Denver. 2024.
- biorxiv. 2024 May 21.
- Research Square Preprint. 2022 Jul.
- Res Sq. 2020 Dec 31:rs.3.rs-100914. [Abstract]
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Cell Proliferation/Viability Assay
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Flow Cytometry
生物活性
製品説明
IC50 & Target
IC50: 26 nM (ERα), 99 nM (ERβ)[1]
体外実験
Bazedoxifene hydrochloride is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene hydrochloride inhibits STAT3 phosphorylation induced by IL-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene hydrochloride (10 μM-20 μM; 2 hours) inhibits STAT3 phosphorylation induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene hydrochloride (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene hydrochloride inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene hydrochloride blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC-1 cells
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Concentration:10 μM, 20 μM
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Incubation Time:2 hours
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Result:Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation.
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Cell Line:Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells
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Concentration:10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC)
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Incubation Time:Overnight
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Result:Induced apoptosis.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female athymic nude mice[2]
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Dosage:5 mg/kg
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Administration:Oral gavage, daily, for 18 days
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Result:Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.
化学情報
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CAS 番号 198480-56-7
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分子量 507.06
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分子式 C30H35ClN2O3
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SMILES
OC1=CC2=C(N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C(C5=CC=C(O)C=C5)=C2C)C=C1.[H]Cl
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別名
TSE-424 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (19)
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Journal Impact Factor
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Most Recent
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Nat Commun
2026 Apr 1;17(1):4716. PMID: 41922346 -
Free Radic Biol Med
IL-6/gp130/STAT3 signaling contributed to the activation of the PERK arm of the unfolded protein response in response to chronic β-adrenergic stimulation. [Abstract]2023 Aug 20:205:163-174. PMID: 37307935 -
J Med Chem
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]2020 Oct 8;63(19):11085-11099. PMID: 32886512 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
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Eur J Pharmacol
Bazedoxifene attenuates intestinal injury in sepsis by suppressing the NF-κB/NLRP3 signaling pathways. [Abstract]2023 May 15:947:175681. PMID: 36965746 -
Glia
Remyelination in neuromyelitis optica spectrum disorder is promoted by edaravone through mTORC1 signaling activation. [Abstract]2023 Feb;71(2):284-304. PMID: 36089914 -
Sci Rep
Novel soluble bazedoxifene formulation gains antiproliferative and migrastatic effect in squamous cell carcinoma cells. [Abstract]2026 Mar 17. PMID: 41844825 -
iScience
Bazedoxifene rescues hepatocytes from chemically induced oxidative ferroptotic injury in vivo and in vitro by inhibiting protein disulfide isomerase. [Abstract]2026 Feb 6;29(3):114931. PMID: 41782827
Bazedoxifene hydrochloride purchased from MedChemExpress. Usage Cited in: iScience. 2026 Feb 6;29(3):114931. [Abstract]
Protective effect of BAZ against erastin-induced cytotoxicity in BRL-3A cells following exposure to erastin (2 μM) ± increasing concentrations of Bazedoxifene (BAZ) (0, 62.5, 125, 250, 500, 1000 nM) as indicated for 24 h.
Bazedoxifene hydrochloride purchased from MedChemExpress. Usage Cited in: iScience. 2026 Feb 6;29(3):114931. [Abstract]
Calcein-AM/PI staining of live and dead BRL-3A cells after exposure to erastin (2 μM) ± Bazedoxifene (BAZ) (1 μM) for 8 h.
Bazedoxifene hydrochloride purchased from MedChemExpress. Usage Cited in: iScience. 2026 Feb 6;29(3):114931. [Abstract]
iNOS protein levels and its dimer and monomer distribution in BRL-3A cells exposed for 8 h to 2 μM erastin ±1 μM Bazedoxifene (BAZ) for 4 h.
Bazedoxifene hydrochloride purchased from MedChemExpress. Usage Cited in: iScience. 2026 Feb 6;29(3):114931. [Abstract]
Cellular NO levels in BRL-3A cells after 8-h exposure to 2 μM erastin ±1 μM Bazedoxifene (BAZ) by flow cytometry.
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Gynecol Oncol
Constitutively active ESR1 mutations in gynecologic malignancies and clinical response to estrogen-receptor directed therapies. [Abstract]2019 Jul;154(1):199-206. PMID: 30987772 -
mSphere
Bazedoxifene Suppresses Intracellular Mycobacterium tuberculosis Growth by Enhancing Autophagy. [Abstract]2020 Apr 8;5(2):e00124-20. PMID: 32269154 -
Arch Biochem Biophys
Role of protein disulfide isomerase in mediating sulfasalazine-induced ferroptosis in HT22 cells: The PDI-NOS-NO-ROS/lipid-ROS cascade. [Abstract]2025 Jun:768:110366. PMID: 40023379 -
Breast Cancer Res Treat
Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. [Abstract]2020 Jan;179(1):67-77. PMID: 31562570 -
J Cell Biochem
Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]2023 Sep;124(9):1404-1422. PMID: 37566640 -
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Res Sq
Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]2020 Dec 31:rs.3.rs-100914. PMID: 33173861
純度とドキュメンテーション
参考文献
[1]. Barry S Komm, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology. 2005 Sep;146(9):3999-4008. [Content Brief]
[2]. Xiaojuan Wu, et al. Bazedoxifene as a Novel GP130 Inhibitor for Pancreatic Cancer Therapy. Mol Cancer Ther. 2016 Nov; 15(11): 2609–2619. [Content Brief]
ホットトピック
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Topics Protein-Protein Interaction: Therapeutic Target-Beyond Cancer
Protein-protein interactions (PPIs) constitute the molecular framework that organizes signaling networks, gene regulation, metabolism, immunity, and cellular homeostasis.
2026-06-18
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Topics A Review of the Mechanisms and Applications of Protein-Protein Interactions (PPIs)
Protein-protein interactions (PPIs) are physical or functional connections formed by two or more proteins through specific interfaces, and they underlie signal transduction, transcriptional regulation, protein degradation, cell-cycle control, DNA repair, immune recognition, and cell death.
2026-06-18
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