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

A cell-permeable, blood-brain barrier permeable, potent activator of Nurr1/NR4A2-dependent transcription activity in (EC₅₀ = 3.9 nM in MN90 cell line).

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Synonyme: (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

Primary Target: Nurr1/NR4A2
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532722
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
500164-74-9C₂₃H₂₂N₂O₄

Preis & Verfügbarkeit

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5.32722.0001
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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
      Applications
      Biological Information
      Primary TargetNurr1/NR4A2
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      5.32722.0001 04055977281866

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Montarolo, F., 2014. PLoS One. 9, e108791.
      Hintermann, S., et al. 2007. Bioorg. Med. Chem. Lett. 17, 193.

      Broschüre

      Titel
      Neuroscience Solutions for productive research
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision31-July-2015 JSW
      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
      DescriptionA 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number500164-74-9
      Chemical formulaC₂₃H₂₂N₂O₄
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      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.
      Toxicity Standard Handling
      ReferencesMontarolo, F., 2014. PLoS One. 9, e108791.
      Hintermann, S., et al. 2007. Bioorg. Med. Chem. Lett. 17, 193.