Biological Activity
α3β2 full agonist (EC50 = 1.6 μM). Also α3β4 partial agonist (EC50 = 1 μM). Exhibits minimal activity at α4β2 and α4β4. Displays high affinity for α3β4, α4β4, α3β2 and α4β2 (Ki values are 0.62, 7.8, 25 and 55 nM respectively).
Compound Libraries
NS 3861 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 400.29 |
Formula | C12H14BrNS.C4H4O4 |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 216853-60-0 |
PubChem ID | 91826078 |
InChI Key | KXBSQPLWTVQFGJ-WLHGVMLRSA-N |
Smiles | CN1C2CCC1CC(C3=C(Br)C=CS3)=C2.OC(/C=C/C(O)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 40.03 | 100 | |
water | 20.01 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 400.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.5 mL | 12.49 mL | 24.98 mL |
5 mM | 0.5 mL | 2.5 mL | 5 mL |
10 mM | 0.25 mL | 1.25 mL | 2.5 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Harpsøe et al (2013) Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors. J.Biol.Chem. 288 2559 PMID: 23229547
Keywords: NS 3861, supplier, NS3861, alpha3beta2, a3b2, α3β2, alpha3beta4, a3b4, α3β4, agonists, partial, Nicotinic, Receptors, (Other, Subtypes), Nicotinic, Receptors, (Other, Subtypes), Tocris Bioscience