Bazedoxifene acetate
Bazedoxifene, a novel selective estrogen receptor modulator (SERM), has been developed to have favorable effects on bone and the lipid profile while minimizing stimulation of uterine or breast tissues. Two large Phase III clinical trials showed that Bazedoxifene, as well as raloxifene, increased bone mineral density, decreased levels of bone turnover markers, and significantly reduced the risk of new vertebral fractures in postmenopausal women compared with placebo.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 530.65 |
| Cas No. | 198481-33-3 |
| Formula | C32H38N2O5 |
| Synonyms | Viviant, WAY-140424, WAY-TES 424, Conbriza, TSE-424, |
| Solubility | insoluble in H2O; ≥182 mg/mL in DMSO; ≥8.483 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | acetic acid;1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.CC(=O)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
MCF-7 human mammary carcinoma cells |
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Preparation method |
Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10−8 to 10−6 M Bazedoxifene acetate for 24 hours. |
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Applications |
Bazedoxifene acetate down-regulates ERα protein in MCF-7:5C and MCF-7:2A Cells. It also inhibits ERα transcriptional activity, blocks cell cycle progression in MCF-7:5C cells and down-regulates cyclin D1. |
| Animal experiment [2]: | |
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Animal models |
Sprague Dawley rats |
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Dosage form |
0.1, 0.3, 1.0, and 3.0 mg/kg per day for 6 weeks |
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Preparation method |
Bazedoxifene was administered orally in a saline, Tween-80, methylcellulose vehicle. |
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Application |
Dose response data for Bazedoxifene acetate demonstrate consistent, significant increased bone mass, compared with control animals via pQCT evaluation is achieved at 0.1 mg/kg per day with increases at 0.3, 1.0, and 3.0 mg/kg per day. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Lewis-Wambi JS, Kim H, Curpan R, Grigg R, Sarker MA, Jordan VC. The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1. Mol Pharmacol. 2011 Oct;80(4):610-20. 2. Komm BS, Kharode YP, Bodine PV, Harris HA, Miller CP, Lyttle CR. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity.Endocrinology. 2005 Sep;146(9):3999-4008. | |
Quality Control & MSDS
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Chemical structure
