您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > ML314
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:
 
ML314
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。
ML314图片
CAS NO:1448895-09-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
ML314 是一种有效的 NTR1 分子激动剂 (EC50 =1.9 μM);对 NTR2 和 GPR35 表现出良好的选择性,但不刺激 Ca2+ 动员。
Cas No.1448895-09-7
化学名2-cyclopropyl-6,7-dimethoxy-4-[4-(2-methoxyphenyl)-1-piperazinyl]-quinazoline
Canonical SMILESCOC1=C(OC)C=C(C(N2CCN(C3=CC=CC=C3OC)CC2)=NC(C4CC4)=N5)C5=C1
分子式C24H28N4O3
分子量420.5
溶解度DMSO: >100mM
储存条件Store at -20°C
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

ML314 is a potent molecule agonist of NTR1 (EC50 = 1.9 μM); showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization.IC50 value: 1.9 uM (EC50) [1]Target: NTR1 agonistMedicinal chemistry optimization of MLS-0233108 led to ML314, the most potent molecule in this second series that exhibited full agonist behavior (100 %) on NTR1 (EC50 = 1.9 μM). ML314 showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization. ML314 is potentially a biased agonist operating via the β-arrestin pathway rather than the traditional Gq coupled pathway. Signaling mediated by β-arrestin has distinct biochemical and functional consequences that may lead to physiological advantages as described below. This probe report describes the discovery and properties of ML301 and summarizes the HTS and follow-up campaign, which identified ML314.

References:
[1]. Hershberger P, et al. Small Molecule Agonists for the Neurotensin 1 Receptor (NTR1 Agonists). Probe Reports from the NIH Molecular Libraries Program