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Merck

P0043

Sigma-Aldrich

PNU-120596

≥98% (HPLC)

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C13H14ClN3O4
CAS-Nummer:
Molekulargewicht:
311.72
MDL-Nummer:
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

solid

Farbe

white to off-white

Löslichkeit

DMSO: >10 mg/mL

Lagertemp.

room temp

SMILES String

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)

InChIKey

CEIIEALEIHQDBX-UHFFFAOYSA-N

Biochem./physiol. Wirkung

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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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
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
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
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

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