EMD527040
目录号: PL14873 纯度: ≥99%
CAS No. :851333-14-7
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中文名称
EMD527040
英文名称
EMD527040
英文别名
β-Alanine, N-[1-oxo-5-(2-pyridinylamino)pentyl]-O-(phenylmethyl)-L-seryl-3-(3,5-dichlorophenyl)-;EMD527040
Cas No.
851333-14-7
分子式
C29H32Cl2N4O5
分子量
587.49
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
EMD527040 是一种高效和高选择性的 αvβ6 拮抗剂,具有抗纤维化活性。EMD527040 可用于肝癌和肝纤维化研究。
生物活性
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research.
性状
Solid
IC50 & Target[1][2]
αvβ6 6 nM (IC50)
体外研究(In Vitro)
EMD527040 inhibits binding of recombinant αvβ6 to fibronectin at 6 nM as compared to >9.5 μM for αvβ3 and αvβ5 integrins (IC5050).
EMD527040 inhibits the attachment of αvβ6 expressing cells (UCLAP3 cells) to fibronectin at IC50 of 1.6 μM, as compared to >50 μM for αvβ3 and αvβ5 integrins.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
EMD527040 (intraperitoneal injection; 20-60 mg/kg; week 2 to 6 after BDL) attenuates bile ductular proliferation and peribiliary collagen deposition by 40-50%, induces downregulation of fibrogenic and upregulation of fibrolytic genes, and improves liver architecture and function. EMD527040 significantly reduced liver and spleen weights by 22% and 50%, respectively in Mdr2(Abcb4) mice.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Eleonora Patsenker, et al. Inhibition of integrin alphavbeta6 on cholangiocytes blocks transforming growth factor-beta activation and retards biliary fibrosis progression. Gastroenterology. 2008 Aug;135(2):660-70.
[2]. Yury Popov, et al. Integrin alphavbeta6 is a marker of the progression of biliary and portal liver fibrosis and a novel target for antifibrotic therapies. J Hepatol
溶解度数据
In Vitro: DMSO : 100 mg/mL (170.22 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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