Bazedoxifene acetate
Based on 17 publication(s) in Google Scholar
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.97%
- CAS No.: 198481-33-3
- 화학식: C32H38N2O5
- 분자량:530.65
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Bazedoxifene acetate
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. 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]
- University of Colorado Denver. 2024.
- biorxiv. 2024 May 21.
- Research Square Preprint. 2022 Jul.
- Res Sq. 2020 Dec 31:rs.3.rs-100914. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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IF
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WB
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Flow Cytometry
Biological Activity
IC50: 26 nM (ERα), 99 nM (ERβ)[1]
Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene acetate 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.
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.
Chemical Information
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CAS No. 198481-33-3
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Appearance Solid
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분자량 530.65
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화학식 C32H38N2O5
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Color White to off-white
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SMILES
CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=CC=C(O)C=C51.CC(O)=O
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Synonyms
TSE-424 acetate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (17)
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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 -
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 acetate 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 acetate 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 acetate 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 acetate 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
용액&용해도
DMSO : ≥ 100 mg/mL (188.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (281 KB)
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SDS (396 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8845 mL | 9.4224 mL | 18.8448 mL | 47.1120 mL |
| 5 mM | 0.3769 mL | 1.8845 mL | 3.7690 mL | 9.4224 mL | |
| 10 mM | 0.1884 mL | 0.9422 mL | 1.8845 mL | 4.7112 mL | |
| 15 mM | 0.1256 mL | 0.6282 mL | 1.2563 mL | 3.1408 mL | |
| 20 mM | 0.0942 mL | 0.4711 mL | 0.9422 mL | 2.3556 mL | |
| 25 mM | 0.0754 mL | 0.3769 mL | 0.7538 mL | 1.8845 mL | |
| 30 mM | 0.0628 mL | 0.3141 mL | 0.6282 mL | 1.5704 mL | |
| 40 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1778 mL | |
| 50 mM | 0.0377 mL | 0.1884 mL | 0.3769 mL | 0.9422 mL | |
| 60 mM | 0.0314 mL | 0.1570 mL | 0.3141 mL | 0.7852 mL | |
| 80 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL | |
| 100 mM | 0.0188 mL | 0.0942 mL | 0.1884 mL | 0.4711 mL |
Bazedoxifene acetate Related Classifications
HY-A0036 Related Classifications
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