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Merck

5.32722

Sigma-Aldrich

Nurr1 Activator, IP7e

Synonym(e):

Nurr1 Activator, IP7e, (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

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About This Item

Empirische Formel (Hill-System):
C23H22N2O4
CAS-Nummer:
Molekulargewicht:
390.43
MDL-Nummer:
UNSPSC-Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Qualitätsniveau

Form

solid

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze

Farbe

off-white

Löslichkeit

DMSO: 50 mg/mL

Lagertemp.

2-8°C

Allgemeine Beschreibung

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

Biochem./physiol. Wirkung

Cell permeable: yes
Primary Target
Nurr1/NR4A2

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.

Sonstige Hinweise

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

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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