NS-6740 hydrochloride
NS-6740 hydrochloride is a partial agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 hydrochloride also acts as a potent modulator of the cholinergic anti-inflammatory pathway. NS-6740 hydrochloride alters the signaling pattern of α7 in an ion channel-independent manner, thereby reducing synaptic function. NS-6740 hydrochloride induces the desensitized state of α7 nAChR. NS-6740 hydrochloride generates robust nAChR-mediated currents. NS-6740 hydrochloride reduces LPS (HY-D1056)-induced TNF-α release from microglia. NS-6740 hydrochloride can be used in the research of neuroinflammation and neuropathic pain.
For research use only. We do not sell to patients.
- CAS No.: 753499-14-8
- Formula: C19H20ClF3N2O2
- Molecular Weight:400.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
NS-6740 (0.01-100 μM; 4.5 h) hydrochloride reduces LPS-induced TNF-α release from primary rat microglia-enriched cultures, with significant inhibition at 25 μM and complete inhibition at 50 and 100 μM[1].
NS-6740 (5 μM; 60 s) hydrochloride induces persistent desensitization of human α7 nAChRs expressed in Xenopus laevis oocytes, blocking ACh responses while leaving receptors responsive to activation by the positive allosteric modulator PNU-120596 (HY-12152)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 753499-14-8
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Molecular Weight 400.82
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Formula C19H20ClF3N2O2
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SMILES
O=C(N1CCN2CCC1CC2)C3=CC=C(C4=CC(C(F)(F)F)=CC=C4)O3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Thomsen MS, et al. The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia. J Neuroimmunol. 2012;251(1-2):65-72. [Content Brief]
[2]. Papke RL, et al. NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity. Neurosci Lett. 2018;677:6-13. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NS-6740 hydrochloride Related Classifications
HY-118646A Related Classifications
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- NS-6740
- 753499-14-8
- NS6740
- NS 6740
- nAChR
- TNF Receptor
- acetylcholine
- GluR1+GluR2 AMPA-type glutamate receptors
- dentate gyrus
- TNF-α
- cholinergic anti-inflammatory pathway
- α2β2 nicotinic acetylcholine receptors
- α7 nicotinic acetylcholine receptor
- long-term potentiation
- hippocampal slices
- microglia
- Inhibitor
- inhibitor
- inhibit