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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $72 | In Stock | |
25 mg | $172 | In Stock | |
50 mg | $289 | In Stock | |
100 mg | $463 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
Description | 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[1]. |
Molecular Weight | 284.22 |
Formula | C12H14BrNS |
Cas No. | 216853-59-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (351.84 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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