NS3861

SKU: orb1298032

Description

NS3861 is a high-affinity agonist selectively targeting heteromeric α3β4 and α4β2 nicotinic acetylcholine receptors, yet it uniquely fails to activate α4-containing subtypes. This functional selectivity, influenced by specific β-subunits and a key serine residue, makes it a valuable research tool for studying nAChR pharmacology and neurobiology in both in vitro and in vivo models.

Research Area

Neuroscience

Images & Validation

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Key Properties

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CAS Number	216853-59-7
MW	284.22
Purity	99.40%
Formula	C₁₂H₁₄BrNS
SMILES	CN1C2CCC1C=C(C2)c1sccc1Br
Target	AChR
Solubility	DMSO:100 mg/mL (351.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (14.07 mM)

Bioactivity

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Target IC50

α3β2:1.6 μm(Ki)|α3β4:1 μm(Ki)|α4β4 (1:4):1.9 μm(Ki)|α4β4 (4:1):1.2 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.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Pharmacology, α4β2 nAChR, α3β4 nAChR, NS3861, NS-3861, NS 3861, Inhibitor, inhibit, Patch Clamp, nAChR, Nicotinic acetylcholine receptors, Heteromeric

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Compound Identifiers

PubChem CID

9838728 ↗

Key Properties

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No computed properties available.

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NS3861 (orb1298032)

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CAS Number:	216853-60-0
MW:	400.29
Formula:	C₁₆H₁₈BrNO₄S

NS3861

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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