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P0043

Sigma-Aldrich

PNU-120596

≥98% (HPLC)

Sinónimos:

N-(5-Chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea, NSC 216666

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About This Item

Fórmula empírica (notación de Hill):
C13H14ClN3O4
Número de CAS:
501925-31-1
Peso molecular:
311.72
Número MDL:
MFCD00095313
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
329819995
NACRES:
NA.77

Nivel de calidad

100

Ensayo

≥98% (HPLC)

Formulario

solid

color

white to off-white

solubilidad

DMSO: >10 mg/mL

temp. de almacenamiento

room temp

cadena SMILES

O=C(NC1=NOC(C)=C1)NC2=CC(Cl)=C(OC)C=C2OC

InChI

1S/C13H14ClN3O4/c1-7-4-12(17-21-7)16-13(18)15-9-5-8(14)10(19-2)6-11(9)20-3/h4-6H,1-3H3,(H2,15,16,17,18)

Clave InChI

CEIIEALEIHQDBX-UHFFFAOYSA-N

Acciones bioquímicas o fisiológicas

An allosteric modulator of α7 nicotinic receptors, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholinePNU-120596 is a positive allosteric modulator selective for the α7 nicotinic acetylcholine receptor. PNU-120596 produces no detectable change in currents mediated by α4β2, α3β4, α9α10 nAChRs. It increases channel mean open time, but does not affect ion selectivity. It does not bind at the agonist binding site, but induces conformational changes similar to the natural effector.
PNU-120596 is a positive allosteric modulator of the α7 nicotinic acetylcholine receptor.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
0000218345
0000218346
0000218346
0000218345
0000122074

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C Morel et al.
Molecular psychiatry, 23(7), 1597-1605 (2017-11-21)
Epidemiological studies report strong association between mood disorders and tobacco addiction. This high comorbidity requires adequate treatment but the underlying mechanisms are unknown. We demonstrate that nicotine exposure, independent of drug withdrawal effects, increases stress sensitivity, a major risk factor
Marta Quadri et al.
Molecular pharmacology, 95(1), 43-61 (2018-10-24)
B-973 is an efficacious type II positive allosteric modulator (PAM) of α7 nicotinic acetylcholine receptors that, like 4BP-TQS and its active isomer GAT107, can produce direct allosteric activation in addition to potentiation of orthosteric agonist activity, which identifies it as
Kateryna Uspenska et al.
Neuroscience letters, 656, 43-50 (2017-07-13)
Several nicotinic acetylcholine receptor (nAChR) subtypes are expressed in mitochondria to regulate the internal pathway of apoptosis in ion channel-independent manner. However, the mechanisms of nAChR activation in mitochondria and targeting to mitochondria are still unknown. Nicotine has been shown
Jean-Rémi Godin et al.
Brain, behavior, and immunity, 87, 286-300 (2019-12-25)
Nicotinic acetylcholine receptors (nAChRs) are best known to function as ligand-gated ion channels in the nervous system. However, recent evidence suggests that nicotine modulates inflammation by desensitizing non-neuronal nAChRs, rather than by inducing channel opening. Silent agonists are molecules that
Shakir D AlSharari et al.
Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco, 19(4), 460-468 (2016-11-01)
α7 nicotinic acetylcholine receptors (nAChRs) play an important role in vagus nerve-based cholinergic anti-inflammatory effects. This study was designed to assess the role of α7 nAChRs in dextran sodium sulfate (DSS)-induced colitis in male and female mouse. We first compared
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