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Bazedoxifene acetate

In stock
Catalog No.
A3233
Estrogen receptor modulator
Grouped product items
SizePriceStock Qty
5mg
$168.00
In stock
10mg
$266.00
In stock
25mg
$465.00
In stock
50mg
$756.00
In stock

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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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt530.65
Cas No.198481-33-3
FormulaC32H38N2O5
SynonymsViviant, WAY-140424, WAY-TES 424, Conbriza, TSE-424,
Solubility≥182 mg/mL in DMSO, ≥8.483 mg/mL in EtOH with ultrasonic and warming, <2.49 mg/mL in H2O
Chemical Nameacetic acid;1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol
SDFDownload SDF
Canonical SMILESCC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.CC(=O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

MCF-7 human mammary carcinoma cells

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.

Reacting condition

10−8 to 10−6 M Bazedoxifene acetate for 24 hours.

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]:

Animal models

Sprague Dawley rats

Dosage form

0.1, 0.3, 1.0, and 3.0 mg/kg per day for 6 weeks

Preparation method

Bazedoxifene was administered orally in a saline, Tween-80, methylcellulose vehicle.

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.

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.

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.

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