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Bazedoxifene HCl

现货
Catalog No.
B1519
新的非甾体,基于吲哚的雌激素受体调节剂(SERM)
组合的产品项目
规格价格库存 数量
25mg
¥ 5,580.00
Ship with 10-15 days
50mg
¥ 9,070.00
Ship with 10-15 days
5mg
¥ 2,020.00
Ship with 10-15 days
10mM (in 1mL DMSO)
¥ 3,240.00
Ship with 10-15 days
10mg
¥ 3,190.00
Ship with 10-15 days

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Background

Bazedoxifene HCl is a novel, non-steroidal and indole-based estrogen receptor modulator (SERM). The IC50 value of bazedoxifene against ERα and ERβ is 23 nM and 89 nM, respectively [1,2].

The estrogen receptor (ER) contains two subtypes, ERα and ERβ. ERs are widely expressed in different tissue types such as kidney, brain, bone, heart, prostate, and endothelial cells. Estrogen and the ERs have been involved in most cancers such as breast cancer,ovarian cancer,colon cancer,prostate cancer, and endometrial cancer [3].

In vitro: Bazedoxifene is a selective SERM currently in development for osteoporosis prevention and treatment. Bazedoxifene was the third generation SERM. In cultured breast cancer (bMCF-7) cells, bazedoxifenedidn’t stimulate ERα mediated transcriptional activity and acted as an antagonist to estradiol. Similar results were also seen in other cell lines including CHO (ovarian), HepG2 (hepatic) or GTI-7 (neuronal) with bazedoxifene having no ERα agonist activity and acting as an antagonist to estradiol action [2].Bazedoxifene didn’t stimulate proliferation of MCF-7 cells but inhibited 17β-estradiol-induced proliferation with an IC50 value of 0.19 nM [4].

In vivo:In an immature rat model, bazedoxifene increased uterine wet weight 35% at a dose of 0.5 mg/kg compared to an 85% increase with raloxifene at the same dose and a 300% increase in uterine weight with ethinyl estradiol at a dose of 10 μg/kg. Ovarectomized rats treated with 0.3 mg/d bazedoxifene displayed maintenance of bone mass and bone strength similar to effects seen with 2 μg/d ethinyl estradiol, 3 mg/d raloxifene, or sham operated animals. In an immature rat uterine model, bazedoxifene (0.5 and 5.0 mg/kg) was associated with less increase in uterine wet weight than either ethinyl estradiol (10 μg/kg) or raloxifene (0.5 and 5.0 mg/kg) [4].

References:
[1].  Miller C P, Collini M D, Tran B D, et al. Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens[J]. Journal of medicinal chemistry, 2001, 44(11): 1654-1657.
[2].  Biskobing D M. Update on bazedoxifene: A novel selective estrogen receptor modulator[J]. Clinical interventions in aging, 2007, 2(3): 299.
[3].  Harris H A, Albert L M, Leathurby Y, et al. Evaluation of an estrogen receptor-β agonist in animal models of human disease[J]. Endocrinology, 2003, 144(10): 4241-4249.
[4].  Komm B S, Kharode Y P, Bodine P V N, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity[J]. Endocrinology, 2005, 146(9): 3999-4008.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt507.06
Cas No.198480-56-7
FormulaC30H34N2O3.HCl
Solubility≥25.35mg/mL in DMSO
Chemical Name1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol;hydrochloride
SDFDownload SDF
Canonical SMILESCC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

CHO细胞,HepG2细胞,GT1-7细胞,MCF-7细胞

溶解方法

该化合物在DMSO中的溶解度>25.4mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0.1 pM-10 nM

应用

1.0 nM 17β-雌二醇和bazedoxifene的共同处理在CHO细胞中具有22.0nM的IC50,HepG2细胞中为4.97nM,在GT1-7细胞中为10.0nM。在用肝脂肪酶启动子荧光素酶构建体转染的HepG2细胞中,bazedoxifene作为激动剂,其EC50为100.0nM。 在MCF-7细胞中,17β-雌二醇和bazedoxifene的共同处理剂量依赖性地抑制细胞增殖,IC50为0.19nM。

动物实验[1]:

动物模型

未成熟的大鼠子宫模型

剂量

0.5和5.0mg / kg; 每日一次,持续3 d; 口服给药

应用

在未成熟的大鼠子宫模型中,bazedoxifene(BZA)以0.5mg / kg给药增加了35%的子宫湿重,在5mg / kg时没有显著差异。整个子宫的组织学检查显示,BZA不影响腔内上皮细胞肥大或增生,子宫肌层肥大或管腔膨胀。BZA仅导致腔细胞高度轻微的增加。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Komm B S, Kharode Y P, Bodine P V N, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity[J]. Endocrinology, 2005, 146(9): 3999-4008.

质量控制

质量控制和MSDS

批次:

化学结构

Bazedoxifene HCl