532722 Nurr1 Activator, IP7e - Calbiochem

532722
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₂N₂O₄

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.32722.0001
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          Glass bottle 10 mg
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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
          FormOff-white solid
          Hill FormulaC₂₃H₂₂N₂O₄
          Chemical formulaC₂₃H₂₂N₂O₄
          ReversibleY
          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

          Documentation

          Nurr1 Activator, IP7e - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

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

          Brochure

          Title
          Neuroscience Solutions for productive research
          Data Sheet

          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
          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.