PNU-120596 - Moligand™, 10mM in DMSO , Allosteric modulator of nicotinic acetylcholine receptor α7 subunit, CAS No.501925-31-1, Allosteric modulator of nicotinic acetylcholine receptor α7 subunit

CAS: 501925-31-1 Cat. No.: P409074 Fórmula: C₁₃H₁₄ClN₃O₄ Peso molecular: 311.72

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Nsc 216666 | 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

PNU-120596 (Nsc 216666) is a positive allosteric modulator ofα7 nAChRwithEC50of 216 nM.
In vitro

PNU-120596 increases agonist (Ach)-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. PNU-120596 increases agonists (choline and ACh)-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation of the evoked response in the continued presence of agonist in Xenopus oocytes. PNU-120596 increases the channel mean open time ofα7 nAChRs but has no effect on ion selectivity and relatively little, if any, effect on unitary conductance. When applied to acute hippocampal slices, PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons; this effect is suppressed by TTX, suggesting that PNU-120596 modulates the function of α7 nAChRs located on the somatodendritic membrane of hippocampal interneurons. Besides the positive modulation to α7 nAChR, PNU-120596 induces a profound retardation of the kinetics of desensitization, raising the potential of Ca²⁺-induced toxicity through excessive stimulation of α7 nAChR. PNU-120596 causes changes in cysteine accessibility at the inner beta sheet, transition zone and agonist binding site while binding to α7 nAChR. Binding sites for PNU-120596 are not in the agonist-binding sites and PNU-120596 enhances agonist-evoked gating of nicotinic receptors by eliciting conformational effects that are similar but nonidentical to the gating conformations promoted by Ach.

In vivo

Systemic administration of PNU-120596 (1 mg/kg) to rats improves the auditory gating deficit caused by amphetamine, a model proposed to reflect a circuit level disturbance associated with schizophrenia. When administered prior to Carrageenan, 30 mg/kg PNU-1230596 significantly blunts mechanical hyperalgesia and weight bearing deficits for up to 4 hours. PNU-120596 attenuates the carrageenan-induced increase in levels of TNF-α and IL-6 within the hindpaw oedema, diclofenac only attenuated IL-6 levels. Established mechanical hyperalgesia induced by Carrageenan or CFA is also partially reversed by PNU-120596.
Cell Data

cell lines：

Concentrations：3-10 μM

Incubation Time：24 hours

Powder Purity:≥99%

Specifications

Sinónimos

Nsc 216666 | 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

ALLOSTERIC MODULATOR

Mecanismo de ação

Allosteric modulator of nicotinic acetylcholine receptor α7 subunit

Nomes e identificadores

SMILES isoméricas

CC1=CC(=NO1)NC(=O)NC2=CC(=C(C=C2OC)OC)Cl

WGK Alemanha

3

Peso molecular

311.72

Reaxy-Rn

11245239

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11245239&ln=

Alvos associados (humanos)

CHRNA7 Tchem Neuronal acetylcholine receptor subunit alpha-7 (4 Activities)

Discover Target: CHRNA7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro DMSO: 59 mg/mL (199.1 mM); Water: Insoluble; Ethanol: Insoluble

Perguntas frequentes

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 501925-31-1, the molecular formula is C13H14ClN3O4, and the molecular weight is 311.72 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.