[CAS NO. 501925-31-1] PNU-120596

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PRODUCTS SPECIFICATIONS [501925-31-1]

Catalog

HY-12152

Brand

MCE

CAS

501925-31-1

DESCRIPTION [501925-31-1]

Overview

MDL	MFCD00095313
Molecular Weight	311.72
Molecular Formula	C13H14ClN3O4
SMILES	O=C(NC1=CC(Cl)=C(C=C1OC)OC)NC2=NOC(C)=C2

For research use only. We do not sell to patients.

Summary

PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC ₅₀ of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research ^[1] .

IC50 & Target

EC50: 216 nM (α7 nAChR) ^[1]

In Vitro

PNU-120596 increases agonist-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. Electrophysiology studies confirme that PNU-120596 increases peak agonist-evoked currents mediated by wild-type receptors and also demonstrates a pronounced prolongation of the evoked response in the continued presence of agonist. PNU-120596 increases the channel mean open time of α7 nAChRs ^[1] .
When applied to acute hippocampal slices, PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents measured in pyramidal neurons ^[1] .
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 ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PNU-120596 (1 mg/kg; intravenous injection; once) treatment improves the auditory gating deficit caused by Amphetamine in rats, a model proposed to reflect a circuit level disturbance associated with schizophrenia ^[1] .
When administered before carrageenan, NU-120596 (30 mg/kg; i.p.) significantly reduces mechanical hyperalgesia and weight-bearing deficits for up to 4 h in Sprague-Dawley rats. PNU-120596 attenuates the carrageenan-induced increase in levels of TNF-α and IL-6 within the hind paw oedema ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague Dawley rats (250-300 g) treated with Amphetamine ^[1]
Dosage:	1 mg/kg
Administration:	Intravenous injection; once
Result:	Improved the auditory gating deficit caused by Amphetamine.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 160.40 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2080 mL	16.0400 mL	32.0801 mL
5 mM	0.6416 mL	3.2080 mL	6.4160 mL
10 mM	0.3208 mL	1.6040 mL	3.2080 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: 2.5 mg/mL (8.02 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (8.02 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Urea, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-

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

NSC 216666

PNU 120596

1-(5-Chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl)-urea

1-(5-Chloro-2,4-dimethoxyphenyl)-3-(5-methyl-1,2-oxazol-3-yl)urea