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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-Bazedoxifene acetate
Bazedoxifene acetate

Chemical Structure : Bazedoxifene acetate

CAS No.: 198481-33-3

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Bazedoxifene acetate (WAY-140424, TSE-424, TSE424)

货号: PC-24542Not For Human Use, Lab Use Only.

Bazedoxifene acetate (TSE-424, WAY-140424) is a potent, orally bioavailable, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM) with IC50 of 23 nM and 99 nM for ERα and ERβ, respectively.

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10 mg ￥580 In stock
25 mg ￥880 In stock
100 mg ￥1580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Bazedoxifene acetate (TSE-424, WAY-140424) is a potent, orally bioavailable, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM) with IC50 of 23 nM and 99 nM for ERα and ERβ, respectively.
Bazedoxifene (TSE-424, WAY-140424) is a high-affinity ligand for ERα (and subsequently for ERβ) with a Ki of 0.1 nM (0.3 nM for ERβ) and no crossover binding to the other members of the steroid/retinoid family of nuclear receptors (e.g., androgen, progesterone, vitamin D, retinoid, rexinoid, etc.).
Bazedoxifene inhibits 17β-estradiol-stimulated proliferation in MCF-7 cells with IC50 of 0.19 nM.
Bazedoxifene reduces raloxifene-stimulated endometrial luminal epithelial cell and myometrial cell hypertrophy.

物理化学性质&存储条件

分子量 530.67
分子式 C32H38N2O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate

参考文献

1. Komm BS, et al. Ann N Y Acad Sci. 2001 Dec;949:317-26.

2. Ronkin S, et al. Obstet Gynecol. 2005 Jun;105(6):1397-404.

3. Komm BS, et al. Endocrinology. 2005 Sep;146(9):3999-4008.

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