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NS3861
🥰Excellent
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
🥰Excellent
Purity: 99.853%
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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $39 | In Stock | In Stock | |
| 10 mg | $72 | In Stock | In Stock | |
| 25 mg | $172 | In Stock | In Stock | |
| 50 mg | $289 | In Stock | In Stock | |
| 100 mg | $463 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.853%
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Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Molecular Weight | 284.22 |
| Formula | C12H14BrNS |
| Cas No. | 216853-59-7 |
| Smiles | CN1C2CCC1C=C(C2)c1sccc1Br |
| Relative Density. | 1.456 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (351.84 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (14.07 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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