AA147

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AA147 是一种小分子内质网 (ER) 蛋白质稳态调节剂。选择性激活未折叠蛋白反应 (UPR) 的 ATF6 臂。

AA147 is a small molecule endoplasmic reticulum (ER) proteostasis regulator.?The selectively activates ATF6 arm of the unfolded protein response (UPR) .It acts as a prodrug that preferentially triggers ATF6 signaling through a mechanism involving localized metabolic activation and selective covalent modification of ER resident proteins that regulate ATF6 activity.

Cell Viability Assay Cell Line:HT22 cells Concentration:0.078, 0.156, 0.312, 0.625, 1.25, 2.5, 5, 10, 20 μMIncubation Time:6 or 16 h (pre-incubation)Result:Showed dose-dependent increases in the viability of glutamate-treated HT22 cells when pretreated with AA147 for 6 or 16 h prior to the glutamate challenge (addition concurrently with the glutamate challenge did not improve the viability of glutamate-treated cells).Reduced ROS accumulation in cells when pre-incubation of 16 h.Cell Viability Assay Cell Line:HT22 cells Concentration:10 μM Incubation Time:16 h Result:Significant increased the expression of genes associated with antioxidant activity in neuronal models, including prolactins and glutathione transferases.Activated NRF2 through a mechanism involving metabolic activation and covalent KEAP1 protein modification.Cell Viability Assay Cell Line:BPAEC Concentration:5, 10 μM Incubation Time:135 h Result:Decreased permeability of cells by activation of ATF6.Western Blot Analysis Cell Line:BPAEC Concentration:5, 10, 15 μM Incubation Time:4, 8, 16, 24, 48 h Result: Significantly induced ATF6 activation and upregulated cofilin phosphorylation (in a concentration-dependent manner).Western Blot Analysis Cell Line:BPAEC Concentration:10 μM Incubation Time:24 h Result: Reduced LPS-induced cATF6 suppression (Fig.5A) and VE-cadherin phosphorylation.

——

ATF6-activator-147

Others

Other Targets

ATF6

——

——

393121-74-9

255.31

C16H17NO2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (195.84 mM)

Cc1ccc(O)c(NC(=O)CCc2ccccc2)c1

——

(-20℃)

With Ice Pack

≥ 2 years