2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. PNU-120596

PNU-120596  (Synonyms: NSC 216666)

Cat. No.: HY-12152 Purity: 99.49%
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PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.

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

PNU-120596 Chemical Structure

PNU-120596 Chemical Structure

CAS No. : 501925-31-1

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10 mM * 1 mL in DMSO
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 USD 49 In-stock
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10 mM * 1 mL in DMSO USD 49 In-stock
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10 mg USD 72 In-stock
50 mg USD 264 In-stock
100 mg USD 468 In-stock
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Based on 1 publication(s) in Google Scholar

PNU-120596 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PNU-120596

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  • Purity & Documentation

  • References

  • Customer Review

Description

PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 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].

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

PNU-120596 Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

311.72

Formula

C13H14ClN3O4
CAS No.
Appearance

Solid

Color

White to gray

SMILES

O=C(NC1=CC(Cl)=C(C=C1OC)OC)NC2=NOC(C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (160.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.49%

COA (248 KB) HNMR (248 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2080 mL 16.0400 mL 32.0801 mL 80.2002 mL
5 mM 0.6416 mL 3.2080 mL 6.4160 mL 16.0400 mL
10 mM 0.3208 mL 1.6040 mL 3.2080 mL 8.0200 mL
15 mM 0.2139 mL 1.0693 mL 2.1387 mL 5.3467 mL
20 mM 0.1604 mL 0.8020 mL 1.6040 mL 4.0100 mL
25 mM 0.1283 mL 0.6416 mL 1.2832 mL 3.2080 mL
30 mM 0.1069 mL 0.5347 mL 1.0693 mL 2.6733 mL
40 mM 0.0802 mL 0.4010 mL 0.8020 mL 2.0050 mL
50 mM 0.0642 mL 0.3208 mL 0.6416 mL 1.6040 mL
60 mM 0.0535 mL 0.2673 mL 0.5347 mL 1.3367 mL
80 mM 0.0401 mL 0.2005 mL 0.4010 mL 1.0025 mL
100 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8020 mL
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PNU-120596 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PNU-120596501925-31-1NSC 216666PNU120596PNU 120596NSC216666NSC-216666nAChRNicotinic acetylcholine receptorsα7nAChRTNF-αIL-6anti-hyperalgesiainflammatorypainneurologicaldisordersInhibitorinhibitorinhibit

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