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Purity: ≥98%
PNU-282987 is a novel, potent and selective agonist of α7 nicotinic acetylcholine receptor(α7 nAChR) with Ki of 26 nM; it has no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget. PNU-282987 evoked whole-cell currents from cultured rat hippocampal neurons that were sensitive to the selective alpha7 nAChR antagonist methyllycaconitine (MLA) and enhanced GABAergic synaptic activity when applied to hippocampal slices.
| ln Vitro |
In rat brain homogenate, PNU-282987 (compound C7) has a Ki of 27 nM and replaces the R7-selective antagonist methylaconitine (MLA) [1]. With an EC50 of 154 nM, PNU-282987 exhibits α7 nAChR agonist activity [1]. Moreover, PNU-282987 blocks 5-HT3 receptors with an IC50 of 4541nM[1].
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| ln Vivo |
Gating deficiencies are reversed by PNU-282987 (compound C7) (iv; 1, 3 mg/kg) [1]. In rat hippocampus neurons, PNU-282987 (30 μM) stimulates currents in a concentration-dependent and MLA-blockable way [1].
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| Animal Protocol |
Animal/Disease Models: Rat[1]
Doses: 1, 3 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: Dramatically reversed amphetamine-induced gating defects. |
| References |
[1]. Alice L Bodnar, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem
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| Molecular Formula |
C14H18CL2N2O
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| Molecular Weight |
301.21
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| CAS # |
123464-89-1
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| Related CAS # |
PNU-282987 S enantiomer free base;737727-12-7;PNU-282987 free base;711085-63-1;(S)-PNU-282987 hydrochloride;128311-08-0
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| SMILES |
O=C(N[ C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3.[H]Cl
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| Chemical Name |
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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: 1 mg/mL (3.32 mM) 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (3.32 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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 50 mg/mL (166.00 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3199 mL | 16.5997 mL | 33.1994 mL | |
| 5 mM | 0.6640 mL | 3.3199 mL | 6.6399 mL | |
| 10 mM | 0.3320 mL | 1.6600 mL | 3.3199 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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