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PNU-120596

SKU: orb1300318

Description

PNU-120596

Research Area

Neuroscience

Images & Validation

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PNU-120596

Key Properties

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CAS Number501925-31-1
MW311.72
Purity98.34%
FormulaC13H14ClN3O4
SMILESCOc1cc(OC)c(NC(=O)Nc2cc(C)on2)cc1Cl
TargetAChR
SolubilityDMSO:31.2 mg/mL (100.09 mM);10% DMSO+90% Corn Oil:2 mg/mL (6.42 mM)

Bioactivity

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Target IC50
α7 nAChR:NA
In Vivo
Systemic administration of PNU-120596 (1 mg/kg) to rats improve 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 attenuate the carrageenan-induced increase in levels of TNF-α and IL-6 withi the hindpaw oedema, diclofenac only attenuated IL-6 levels. Established Mechanical hyperalgesia induced by Carrageenan or CFA is also partially reversed by PNU-120596.
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In Vitro
PNU-120596 increases agonist (Ach)-evoked calcium flux mediated by an engineered variant o the human α7 nAChR. PNU-120596 increases agonists (choline and ACh)-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation o the evoked response in the continued presence of agonist in Xenopus oocytes. PNU-120596 increase 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 increase the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons; this effect is suppressed by TTX, suggesting that PNU-120596 modulate the function of α7 nAChRs located o the somatodendritic membrane of hippocampal interneurons. Beside the positive modulation to α7 nAChR, PNU-120596 induces a profound retardation o the kinetics of desensitization, raisin the potential of Ca2+ induced toxicity through excessive stimulation of α7 nAChR. PNU-120596 causes Changes in cysteine accessibility a 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.
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Cell Research
SH-SY5Y-α7 cells are plated on 96-well plates at a density of 15,000 cells per well (100 μL of 1.5 × 105 cells per mL) in complete growth medium and placed into a 37℃ncubator for 20 to 24 hours. Complete growth medium then is replaced with Experimental medium alone ("PNU-120596 free") or containing appropriate concentration of PNU-120596 and returns to the 37℃cubator for 20 to 24 hours the medium is then replaced with fresh Experimental medium and 20 μL per well MTS solution and returned to the 37℃ncubator for 3 hours, after whic the plate is read on a microplate spectrophotometer at an absorbance of 490 nM. For All data analysis, data are normalized to untreated compound-free wells (100% cell viability) and a background absorbance taken from wells containing Experimental medium and MTS solution.(Only for Reference)
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Animal Research
Animal Models: Male Sprague Dawley rats (weighing 250–300 g)Formulation: PNU-120596 is dissolved in 5% DMSO and 5% Solutol in PBS.Dosages: 1 mg/kgAdministration: PNU-120596 is intravenously administrated 5 minutes before auditory gating measurements.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
DisclaimerFor research use only

Alternative Names

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IL-6, Inhibitor, inhibit, inflammatory, pain, NSC216666, NSC-216666, NSC 216666, nAChR, PNU 120596, PNU120596, PNU-120596, Nicotinic acetylcholine receptors, neurological, anti-hyperalgesia, disorders, α7nAChR, α7 nAChR, TNF-α

Similar Products

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  • PNU-120596

    PNU-120596 [orb1222158]

    >98% (HPLC)

    501925-31-1

    311.7

    C13H14ClN3O4

    1 g, 500 mg, 10 mg, 25 mg, 50 mg, 5 mg, 100 mg, 200 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
311434 ↗

Key Properties

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No computed properties available.

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PNU-120596 (orb1300318)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 ml x 10 mM (in DMSO)
¥ 1,040.00
5 mg
¥ 1,040.00
10 mg
¥ 1,300.00
25 mg
¥ 2,080.00
50 mg
¥ 3,380.00
100 mg
¥ 5,590.00
200 mg
¥ 7,930.00
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