Bazedoxifene
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Bazedoxifene是一种选择性雌激素受体调节剂(SERM),作用于雌激素受体α和β的IC50值分别为26和99 nM [1]。
Bazedoxifene是一种SERM,用于雌激素内源性水平损失引起的绝经后骨质疏松的预防和治疗。其被开发为第三代SERM,可降低脊椎和非脊椎骨折的风险,并且对乳房或子宫无刺激作用。Bazedoxifene是一种雌激素受体的配体,具有基于吲哚的核心结合域。其结合至雌激素受体α(IC50值为23 nM)和ERβ(IC50值为85 nM),在骨、心血管系统和中枢神经系统(CNS)中表现出激动剂活性,而在乳腺和子宫内膜展现出拮抗活性。Bazedoxifene竞争性地抑制17β雌二醇结合至ERα和ERβ [1,2和3]。
在MCF7细胞中,Bazedoxifene治疗未显示出ER激动剂活性并且对细胞增殖没有影响。然而,其抑制17β雌二醇诱导的转录激活和细胞增殖[3]。
在去卵巢大鼠中,0.3或3.0 mg/kg日剂量的Bazedoxifene给药6周引起骨骼保护作用,防止骨质流失并增加骨密度。此外,Bazedoxifene显著改善第五腰椎的压缩强度。另外,3.0 mg/kg日剂量的Bazedoxifene给药对大鼠子宫显示出中等刺激作用,子宫湿重稍有增加。Bazedoxifene对大鼠血管舒缩活动也不具有ER激动剂作用[2,3]。
参考文献:
[1] de Villiers TJ. Bazedoxifene: a novel selective estrogen receptor modulator for postmenopausal osteoporosis. Climacteric. 2010 Jun;13(3):210-8.
[2] Duggan ST, McKeage K. Bazedoxifene: a review of its use in the treatment of postmenopausal osteoporosis. Drugs. 2011 Nov 12;71(16):2193-212.
[3] Kawate H, Takayanagi R. Efficacy and safety of bazedoxifene for postmenopausal osteoporosis. Clin Interv Aging. 2011;6:151-60.
Storage | Store at -20°C |
M.Wt | 470.6 |
Cas No. | 198481-32-2 |
Formula | C30H34N2O3 |
Solubility | Soluble in DMSO |
Chemical Name | 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
Description | Bazedoxifene是一种第三代选择性雌激素受体调节剂。 | |||||
靶点 | estrogen receptor | |||||
IC50 |