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艾曲波帕

血小板生成素受体激动剂

产品号 #(选择产品)

产品号 #100-0250_C

血小板生成素受体激动剂

总览

艾曲波帕是一种血小板生成素受体(TpoR)激动剂(在报告基因实验中EC₅₀ = 0.27µM)和铁螯合剂(Erickson‐Miller et al.)。艾曲波帕和TpoR之间的相互作用可触发人骨髓祖细胞向巨核细胞的增殖和分化,并增加血小板的生长和产生(Erickson‐Miller et al.)。

分化
·刺激原代人CD34+骨髓细胞向CD41+巨核细胞的增殖和分化(Erickson‐Miller et al.)。

别名
SB497115
 
应用
分化
 
CAS 编号
496775-61-2
 
化学式
C₂₅H₂₂N₄O₄
 
分子量
442.5 克/摩尔
 
纯度
≥98%
 
通路
STAT5
 
靶点
TpOR
 

产品说明书及文档

请在《产品说明书》中查找相关支持信息和使用说明,或浏览下方更多实验方案。

Document Type
Product Name
Catalog #
Lot #
Language
Product Name
Eltrombopag
Catalog #
100-0250, 100-0251
Lot #
All
Language
English
Document Type
Safety Data Sheet
Product Name
Eltrombopag
Catalog #
100-0250, 100-0251
Lot #
All
Language
English

相关材料与文献

文献 (1)

Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. C. L. Erickson-Miller et al. Stem cells (Dayton, Ohio) 2009 feb

Abstract

Eltrombopag is a first-in-class, orally bioavailable, small-molecule, nonpeptide agonist of the thrombopoietin receptor (TpoR), which is being developed as a treatment for thrombocytopenia of various etiologies. In vitro studies have demonstrated that the activity of eltrombopag is dependent on expression of TpoR, which activates the signaling transducers and activators of transcription (STAT) and mitogen-activated protein kinase signal transduction pathways. The objective of this preclinical study is to determine if eltrombopag interacts selectively with the TpoR to facilitate megakaryocyte differentiation in platelets. Functional thrombopoietic activity was demonstrated by the proliferation and differentiation of primary human CD34(+) bone marrow cells into CD41(+) megakaryocytes. Measurements in platelets in several species indicated that eltrombopag specifically activates only the human and chimpanzee STAT pathways. The in vivo activity of eltrombopag was demonstrated by an increase of up to 100{\%} in platelet numbers when administered orally (10 mg/kg per day for 5 days) to chimpanzees. In conclusion, eltrombopag interacts selectively with the TpoR without competing with Tpo, leading to the increased proliferation and differentiation of human bone marrow progenitor cells into megakaryocytes and increased platelet production. These results suggest that eltrombopag and Tpo may be able to act additively to increase platelet production.

更多信息

更多信息
Molecular Weight 442.5 g/mol
Alternative Names SB497115
Cas Number 496775-61-2
Chemical Formula C₂₅H₂₂N₄O₄
纯度 ≥ 98%
Target TpOR
Pathway STAT5
质量保证:

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