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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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: Nurr1/NR4A2
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
500164-74-9C₂₃H₂₂N₂O₄

Products

Catalog NumberPackaging Qty/Pack
5.32722.0001 Glass bottle 10 mg
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
Catalog Number GTIN
5.32722.0001 04055977281866

Documentation

Nurr1 Activator, IP7e - CAS 500164-74-9 - 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
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.