AA147

CAS No. 393121-74-9

AA147( ATF6-activator-147 )

Catalog No. M22642 CAS No. 393121-74-9

AA147 is a small molecule endoplasmic reticulum (ER) proteostasis regulator.?The selectively activates ATF6 arm of the unfolded protein response (UPR) .

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    AA147
  • Note
    Research use only, not for human use.
  • Brief Description
    AA147 is a small molecule endoplasmic reticulum (ER) proteostasis regulator.?The selectively activates ATF6 arm of the unfolded protein response (UPR) .
  • Description
    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.
  • In Vitro
    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.
  • In Vivo
    ——
  • Synonyms
    ATF6-activator-147
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    ATF6
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    393121-74-9
  • Formula Weight
    255.31
  • Molecular Formula
    C16H17NO2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (195.84 mM)
  • SMILES
    Cc1ccc(O)c(NC(=O)CCc2ccccc2)c1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Christina COOLEY, et al. Regulators of the endoplasmic reticulum proteostasis network. WO2017117430A1.
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