NS3861

Research use only, not for human use.

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and bind with high affinity to heteromeric α3β4 and α4β2 nAChRs.

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and bind with high affinity to heteromeric α3β4 and α4β2 nAChRs. NS3861 displays the β-subunit preference and a complete lack of activation at α4-containing receptors. The maximal efficacy of NS3861 appeared solely dependent on the nature of the ligand-binding domain. Furthermore, a principal subunit serine to threonine substitution may explain the lack of NS3861 activation at α4-containing receptors.(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.

NS3861 displays the opposite β-subunit preference and a complete lack of activation at α4-containing receptors in HEK293 cell lines. NS3861 selectively activates α3- but not α4-containing nAChRs and it displays higher efficacy at the α3β2 receptor compared with the α3β4 receptor, with EC50s of 1.7 and 0.15 μM for α3β2 and α3β4 receptor, respectively. NS3861 shows high affinity and partial agonist properties in α3β4-expressed nAChRs.

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Cell Cycle/DNA Damage

AChR

CXCR3

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216853-59-7

284.22

C12H14BrNS

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (175.92 mM)

CN1C2CCC1C=C(C2)c1sccc1Br

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(-20℃)

With Ice Pack

≥ 2 years