NS-6740 hydrochloride
NS-6740 hydrochloride is a silent agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 hydrochloride reduces LPS-induced TNF-α release and regulates the cholinergic anti-inflammatory pathway. NS-6740 hydrochloride exerts anti-inflammatory effects. NS-6740 hydrochloride reduces long-term potentiation in hippocampal brain slices. NS-6740 hydrochloride can be used in research related to neuroinflammation and schizophrenia.
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
NS-6740 (0.01-100 μM; 30 min) hydrochloride potently inhibits LPS-induced TNF-α release in enriched primary rat microglial cultures, achieving complete inhibition at concentrations of 50 and 100 μM. Co-treatment with a partial α7 nAChR agonist enhances this effect, which is not mediated by regulation of the MAPK pathway[1].
NS-6740 (5 μM; 60 s) hydrochloride induces persistent desensitization of α7 nAChR expressed in Xenopus laevis oocytes, and the desensitized receptors can be activated by the positive allosteric modulator PNU-120596 (HY-12152)[2].
NS-6740 hydrochloride acts as an antagonist of the recombinant 5-HT3A receptor expressed in HEK293 cells, with an IC50 value of 4827 nM[3].
NS-6740 hydrochloride binds to native rat α7 nAChR with high affinity, with a Ki value of 2.85 nM[3].
NS-6740 hydrochloride inhibits the activation of recombinant rat α7 nAChRs expressed in HEK293 cells induced by BMS-933043 (HY-W062702), with an IC50 value of 283 nM for peak current and 255 nM for net charge[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NS-6740 (3-10 mg/kg; s.c.; single dose) hydrochloride, at doses achieving 89% and 98% α7 nAChR occupancy, does not enhance memory retention in the mouse novel object recognition task[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 (male, 25-30g)[3]
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Dosage:10 mg/kg
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Administration:s.c.; single dose
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Result:Abolished the improved discrimination index seen in mice treated with BMS-933043 alone.
Achieved 98% α7 nAChR occupancy in mouse forebrain, with an average brain/plasma ratio >8.
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Animal Model:C57Bl/6 (male, 25-30g)[3]
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Dosage:3-10 mg/kg
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Administration:s.c.; single dose
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Result:Did not improve 24-hour novel object recognition memory in mice at 3 mg/kg and 10 mg/kg.
Achieved 89% α7 nAChR occupancy in mouse forebrain at 3 mg/kg, with an average brain/plasma ratio >8.
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. Journal of neuroimmunology. 2012 Oct 15;251(1-2):65-72. [Content Brief]
[2]. Papke RL, et al. NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity. Neuroscience letters. 2018 Jun 11;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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