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ML161
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML161图片
CAS NO:423735-93-7
规格:98%
分子量:361.23
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
PAR1 inhibitor
CAS:423735-93-7
分子式:C17H17BrN2O2
分子量:361.23
纯度:98%
存储:Store at -20°C

Background:

ML161 is a selective inhibitor of PAR1 with IC50 value of 0.26 μM [1].


Protease-activated receptor-1(PAR-1) is a unique G-protein-coupled receptor belonging to the protease-activated receptor family and its activation leads to downstream signaling events that launch a variety of cellular responses related to tumor progression [1].


ML161 is a potent PAR1 inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with human platelets, ML161 treatment inhibited the activation of thrombin-induced platelet in a dose-dependent manner by detecting P-selectin expression [1]. When tested with granule secretion, ML161 exhibited a potent inhibition on P-selectin expression in a dose-dependent manner with EC50 value of 0.3μM and also inhibited SFLLRN-induced thrombus formation [2].


参考文献:
[1].  Dockendorff, C., et al., Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett, 2012. 3(3): p. 232-237.
[2].  VerPlank, L., et al., Chemical Genetic Analysis of Platelet Granule Secretion-Probe 3, in Probe Reports from the NIH Molecular Libraries Program. 2010, National Center for Biotechnology Information (US): Bethesda (MD).