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532722 Nurr1 Activator, IP7e - CAS 500164-74-9 - Calbiochem

Descripción

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CAS #Empirical Formula
500164-74-9C₂₃H₂₂N₂O₄

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      Description
      OverviewA cell-permeable, isoxazolopyridinone compound that acts as a potent activator of Nurr1/NR4A2-dependent transcription activity in reporter assays using Nurr1-expressing murine midbrain dopaminergic neuronal cell line MN9D (EC50 = 3.9 nM, Emax = 2.1-fold of basal activity) and exhibits oral availability as well as blood-brain-barrier permeability in mice. Preventive treatment (10 mg/kg/12h from 7th to 23rd day post MOG35-55 immunization) is shown to delay the onset (15 d.p.i. with & 12 d.p.i. without preventive treatment) and severity of experimental autoimmune encephalomyelitis (EAE) in a murine multiple sclerosis (MS) model in vivo, while no improvement of EAE symptoms is observed if the treatment starts after the disease onset (10 mg/kg/12h from 21 d.p.i. to 36 d.p.i.). Consistent with the known negative regulating role of Nurr1 against NF-κB pathway, preventive treatment is shown to result in significantly reduced expression of 16 NF-κB pathway genes in the spinal cord of EAE mice.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532722
      Brand Family Calbiochem®
      Synonyms(6-(4-((2-Methoxyethoxy)methyl)phenyl)-5-methyl-3-phenylisoxazolo(4,5-c)pyridin-4(5H)-one), 6-(4-((2-Methoxyethoxy)methyl)phenyl)-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one, Isoxazolo-Pyridinone 7e, NR4A2 Activator
      References
      ReferencesMontarolo, F., 2014. PLoS One. 9, e108791.
      Hintermann, S., et al. 2007. Bioorg. Med. Chem. Lett. 17, 193.
      Product Information
      CAS number500164-74-9
      FormOff-white solid
      Hill FormulaC₂₃H₂₂N₂O₄
      Chemical formulaC₂₃H₂₂N₂O₄
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetNurr1/NR4A2
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Número de referencia GTIN
      5.32722.0001 04055977281866