您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > ML161
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
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
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
ML161 (ML161) 是蛋白酶激活受体 1 (PAR1) 的变构抑制剂，IC50 为 0.26 μM.
Cas No.423735-93-7
化学名2-bromo-N-[3-(butanoylamino)phenyl]benzamide
Canonical SMILESCCCC(=O)NC1=CC=CC(=C1)NC(=O)C2=CC=CC=C2Br
分子式C17H17BrN2O2
分子量361.23
溶解度≥ 16.4mg/mL in DMSO, ≥ 46.9 mg/mL in EtOH with ultrasonic
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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).