Bazedoxifene hydrochloride (TSE-424 hydrochloride) 能透过血脑屏障的，非甾体、选择性的雌激素受体调节剂 (SERM)，对 ERα 和 ERβ 作用的 IC50 值分别为 26 nM 和 99 nM，可用于骨质疏松症的研究。Bazedoxifene hydrochloride 也是一种 IL-6/GP130 蛋白相互作用抑制剂，可用于胰腺癌的研究。 Information Bazedoxifene HCl (WAY-140424, TSE-424) is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to bothERαandERβwithIC50of 23 nM and 89 nM, respectively. Targets ERα (radioligand binding assay); ERβ (radioligand binding assay) 23 nM; 89 nM In vitro Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene does not stimulate ERα mediated transcriptional activity and acts as an antagonist to estradiol in cultured breast cancer (bMCF-7) cells. Similar results are 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. Bazedoxifene does not stimulate proliferation of MCF-7 cells but did inhibit 17β-estradiol-induced proliferation with IC50 of 0.19 nM. In vivo In an immature rat model, bazedoxifene increases 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. Cell Research(from reference) Cell lines：MCF-7 Concentrations：~10 nM Incubation Time：7 days
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Bazedoxifene (WAY-140424) HCl
Dangerous GoodsCAS number：198480-56-7 molecular formula：C30H34N2O3.HCl
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | TSE-424 (hydrochloride) | YHA48056 | BCP28606 | PF-05208749 HCl | 1H-Indol-5-ol, 1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-, hydrochloride (1:1) | DTXSID80433034 | Bazedoxifene HCl | SW219560-1 | E98952 | HY-A00 | ||
| CAS number | 198480-56-7 | molecular formula | C30H34N2O3.HCl |
| molecular weight | 507.06 g/mol | Exact mass | - |
| PSA | 57.900 Ų | logp | - |
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physicochemical properties
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Safety information
pictogram：
GHS08
Signal word：
Danger
Hazard Statement：
H360: 可能损害生育力或未出生的孩子
Statement of Preventive Measures：
P405: 密闭存放 P501: 将内容物/容器处理到。。。 P201: 使用前获取特殊说明 P308+P313: 如接触到或有疑虑：求医/就诊。 P281: 根据需要使用个人防护设备。 P202: 在阅读并理解所有安全预防措施之前，不要进行操作。
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