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Purity: ≥98%
PNU-120596 (PNU120596; NSC 216666; PNU 120596; NSC-216666) is a potent and selective PAM (positive allosteric modulator) of α7 nAChR (acetylcholine receptor) with an EC50 of 216 NM.
| ln Vitro |
PNU-120596 enhances agonist-induced calcium polarization, which is facilitated by engineered human α7 nAChR variations. According to electrophysiological investigations, PNU-120596 enhanced wild-type lead-mediated increases in cardiac agent-evoked currents and greatly lengthened the evoked response when the agonist was present. The average channel open time of α7 nAChR is increased by PNU-120596 [1]. PNU-120596 has been shown to increase the frequency of ACh-evoked GABA postsynaptic currents recorded in pyramidal neurons in hippocampus slices over time [1]. Through conformational effects akin to but separate from the ACh-promoted gating conformation, PNU-120596 improves agonist-induced nicotine uptake gating [2].
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| ln Vivo |
Rats with amphetamine-induced abnormalities in auditory gating are treated with PNU-120596 (1 mg/kg; i.v.; once) to improve the model's representation of circuit-level disruptions linked to schizophrenia [1]. When given prior to carryeenan, NU-120596 (30 mg/kg; i.p.) dramatically decreased mechanical hyperalgesia and weight-bearing deficits in Sprague-Dawley rats for as long as four hours. PNU-120596 reduces the rise in TNF-α and IL-6 in hindpaw edema caused by carrageenan [3].
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| Animal Protocol |
Animal/Disease Models: Male Sprague Dawley rats (250-300 g) treated with Amphetamine[1]
Doses: 1 mg/kg Route of Administration: intravenous (iv) injection; once Experimental Results: Improved the auditory gating deficit caused by Amphetamine. |
| References |
[1]. Hurst RS, et al. A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci, 2005, 25(17), 4396-4405.
[2]. Barron SC, et al. An allosteric modulator of alpha7 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 acetylcholine. Mol Pharmacol, 2009 76(2), 253-263. [3]. Munro G, et al. The α7 nicotinic ACh receptor agonist compound B and positive allosteric modulator PNU-120596 both alleviate inflammatory hyperalgesia and cytokine release in the rat. Br J Pharmacol, 2012, doi: 10.1111/j.1476-5381.2012.02003.x |
| Molecular Formula |
C13H14CLN3O4
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| Molecular Weight |
311.72
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| CAS # |
501925-31-1
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| Related CAS # |
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| SMILES |
ClC1=C(C([H])=C(C(=C1[H])N([H])C(N([H])C1C([H])=C(C([H])([H])[H])ON=1)=O)OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
CEIIEALEIHQDBX-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
1-(5-Chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 10 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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