| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | DMSO. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide.
- CAS number: 123464-89-1
- Molecular formula: C14H17ClN2O.
- Purity: >98%
- Concentration: EC50 ~ 5 μM.
- Form: Lyophilized powder.
- Solubility: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: α7 nAChR
- Source: Synthetic
- Activity: PNU 282987 is a selective agonist of α7 nicotinic acetylcholine receptor (nAChR)1-2, with an EC50 of 5.6 μM in Xenopus oocytes3 and Ki of 26 nM in rat α7 nAChR1. Via modulating/enhancing hippocampal GABAergic neurotransmission, PNU 282987 improves auditory gating and enhances hippocampal oscillatory activity and therefore may offer a potential pharmacotherapy in the treatment of schizophrenia1.
Scientific background
Nicotinic acetylcholine receptors (nAChRs) are members of the Cys-Loop ligand-gated ion channel superfamily, located both in the peripheral and central nervous systems (PNS and CNS, respectively). These receptors, existing as both homopentameric and heteropentameric transmembrane ion channels, are validated therapeutic targets for various CNS pathologies1.PNU 282987 is a selective agonist of α7 nAChRs2-3, which are predominantly found in the central nervous system. It enhances α7 nAChRs currents with an EC50 of 5.6 µM in Xenopus oocytes4 and has a Ki of 26 nM in rat α7 nAChR2. Selective α7 nAChR agonists, such as PNU 282987, improve performance in sensory gating, novel object recognition, social recognition, water maze performance, or inhibitory avoidance models of cognitive function4. Given these roles, targeting α7 nAChRs has been considered as a viable strategy for a variety of diseases involving cognitive deficits and neurodegeneration5-6.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
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