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NS3861

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Catalog No. T9542Cas No. 216853-59-7

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) that binds with high affinity to heteromeric α3β4 and α4β2 nAChRs, displaying β-subunit preference and no activation at α4-containing receptors. The maximal efficacy of NS3861 depends on the ligand-binding domain, and a serine to threonine substitution in the principal subunit may explain the lack of activation at α4-containing receptors.

NS3861

NS3861

🥰Excellent
Purity: 99.40%
Catalog No. T9542Cas No. 216853-59-7
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) that binds with high affinity to heteromeric α3β4 and α4β2 nAChRs, displaying β-subunit preference and no activation at α4-containing receptors. The maximal efficacy of NS3861 depends on the ligand-binding domain, and a serine to threonine substitution in the principal subunit may explain the lack of activation at α4-containing receptors.
Pack SizePriceAvailabilityQuantity
5 mg$39In Stock
10 mg$72In Stock
25 mg$172In Stock
50 mg$289In Stock
100 mg$463In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Purity:99.40%
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Product Introduction

Bioactivity
Description
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) that binds with high affinity to heteromeric α3β4 and α4β2 nAChRs, displaying β-subunit preference and no activation at α4-containing receptors. The maximal efficacy of NS3861 depends on the ligand-binding domain, and a serine to threonine substitution in the principal subunit may explain the lack of activation at α4-containing receptors.
Targets&IC50
α4β4 (4:1):1.2 μm(Ki), α3β2:1.6 μm(Ki), α3β4:1 μm(Ki), α4β4 (1:4):1.9 μm(Ki)
In vitro
NS3861 was found to activate wild-type α3β4 nAChRs (Figs. 3R and 4) but did not activate wild-type α4β2. Whereas NS3861 was a partial agonist at α3β4, it proved to be a full agonist at α3β2 albeit with ~10-fold lower potency consistent with the binding affinities. Efficacy at the α3/α4 + β4/β2 receptor was almost identical to that of wild-type α3β4, whereas no efficacy could be seen at α4/α3 + β2/β4[1].
Chemical Properties
Molecular Weight284.22
FormulaC12H14BrNS
Cas No.216853-59-7
SmilesCN1C2CCC1C=C(C2)c1sccc1Br
Relative Density.1.456 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (351.84 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.5184 mL17.5920 mL35.1840 mL175.9201 mL
5 mM0.7037 mL3.5184 mL7.0368 mL35.1840 mL
10 mM0.3518 mL1.7592 mL3.5184 mL17.5920 mL
20 mM0.1759 mL0.8796 mL1.7592 mL8.7960 mL
50 mM0.0704 mL0.3518 mL0.7037 mL3.5184 mL
100 mM0.0352 mL0.1759 mL0.3518 mL1.7592 mL

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