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Merck

5.32722

Nurr1 Activator, IP7e

동의어(들):

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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크기 선택


제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C23H22N2O4
CAS 번호:
Molecular Weight:
390.43
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
기술 서비스
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도움 문의
기술 서비스
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도움 문의

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

off-white

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Nurr1/NR4A2

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

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

Preparation Note

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.

Legal Information

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

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


시험 성적서(COA)

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