NS-6740
Based on 1 Customer Validation
NS-6740 is a silent agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 reduces LPS-induced TNF-α release and regulates the cholinergic anti-inflammatory pathway. NS-6740 exerts anti-inflammatory effects. NS-6740 reduces long-term potentiation in hippocampal brain slices. NS-6740 can be used in research related to neuroinflammation and schizophrenia.
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- Pureza : 99.93%
- No. CAS: 753500-02-6
- Fòrmula: C19H19F3N2O2
- Peso molecular:364.36
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4827 nM
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Inhibition of recombinant human 5-HT3A receptor function in HEK293 cells measured by calcium flux (FLIPR) assay.
Inhibition of recombinant human 5-HT3A receptor function in HEK293 cells measured by calcium flux (FLIPR) assay.
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27467081 |
| HEK293 | IC50 |
283 nM
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Inhibition of BMS-933043-elicited peak current response in HEK293 cells expressing recombinant rat α7 nAChRs measured by whole cell voltage clamp electrophysiology, with pre-incubation for 1 or 2 min.
Inhibition of BMS-933043-elicited peak current response in HEK293 cells expressing recombinant rat α7 nAChRs measured by whole cell voltage clamp electrophysiology, with pre-incubation for 1 or 2 min.
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27467081 |
| HEK293 | IC50 |
255 nM
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Inhibition of BMS-933043-elicited net charge crossing the membrane in HEK293 cells expressing recombinant rat α7 nAChRs measured by whole cell voltage clamp electrophysiology, with pre-incubation for 1 or 2 min.
Inhibition of BMS-933043-elicited net charge crossing the membrane in HEK293 cells expressing recombinant rat α7 nAChRs measured by whole cell voltage clamp electrophysiology, with pre-incubation for 1 or 2 min.
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27467081 |
In Vitro
NS-6740 (0.01-100 μM; 30 min) 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) 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 acts as an antagonist of the recombinant 5-HT3A receptor expressed in HEK293 cells, with an IC50 value of 4827 nM[3].
NS-6740 binds to native rat α7 nAChR with high affinity, with a Ki value of 2.85 nM[3].
NS-6740 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), 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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No. CAS 753500-02-6
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Appearance Oil
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Peso molecular 364.36
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Fòrmula C19H19F3N2O2
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Color Colorless to off-white
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SMILES
O=C(C1=CC=C(O1)C2=CC=CC(C(F)(F)F)=C2)N3CCN4CCC3CC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 12.5 mg/mL (34.31 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7445 mL | 13.7227 mL | 27.4454 mL | 68.6135 mL |
| 5 mM | 0.5489 mL | 2.7445 mL | 5.4891 mL | 13.7227 mL | |
| 10 mM | 0.2745 mL | 1.3723 mL | 2.7445 mL | 6.8613 mL | |
| 15 mM | 0.1830 mL | 0.9148 mL | 1.8297 mL | 4.5742 mL | |
| 20 mM | 0.1372 mL | 0.6861 mL | 1.3723 mL | 3.4307 mL | |
| 25 mM | 0.1098 mL | 0.5489 mL | 1.0978 mL | 2.7445 mL | |
| 30 mM | 0.0915 mL | 0.4574 mL | 0.9148 mL | 2.2871 mL |
NS-6740 Related Classifications
HY-118646 Related Classifications
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