NS3861 fumarate
Based on 1 publication(s) in Google Scholar
NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 216853-60-0
- Formula: C16H18BrNO4S
- Molecular Weight:400.29
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NS3861 fumarate
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Biological Activity
NS3861 fumarate displays the opposite β-subunit preference and a complete lack of activation at α4-containing receptors in HEK293 cell lines. NS3861 fumarate 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[1].
NS3861 fumarate shows high affinity and partial agonist properties in α3β4-expressed nAChRs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 216853-60-0
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Appearance Solid
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Molecular Weight 400.29
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Formula C16H18BrNO4S
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Color White to off-white
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SMILES
BrC1=C(C2=CC(CC3)N(C)C3C2)SC=C1.OC(/C=C/C(O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
Nicotinic acetylcholine receptors modulate casein secretion and claudin expression in mammary epithelial cells by regulating STAT5 and Akt pathways. [Abstract]2025 Jul 12:770:152036. PMID: 40382844
Solvent & Solubility
DMSO : 100 mg/mL (249.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4982 mL | 12.4909 mL | 24.9819 mL | 62.4547 mL |
| 5 mM | 0.4996 mL | 2.4982 mL | 4.9964 mL | 12.4909 mL | |
| 10 mM | 0.2498 mL | 1.2491 mL | 2.4982 mL | 6.2455 mL | |
| 15 mM | 0.1665 mL | 0.8327 mL | 1.6655 mL | 4.1636 mL | |
| 20 mM | 0.1249 mL | 0.6245 mL | 1.2491 mL | 3.1227 mL | |
| 25 mM | 0.0999 mL | 0.4996 mL | 0.9993 mL | 2.4982 mL | |
| 30 mM | 0.0833 mL | 0.4164 mL | 0.8327 mL | 2.0818 mL | |
| 40 mM | 0.0625 mL | 0.3123 mL | 0.6245 mL | 1.5614 mL | |
| 50 mM | 0.0500 mL | 0.2498 mL | 0.4996 mL | 1.2491 mL | |
| 60 mM | 0.0416 mL | 0.2082 mL | 0.4164 mL | 1.0409 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3123 mL | 0.7807 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2498 mL | 0.6245 mL |
NS3861 fumarate Related Classifications
HY-110121 Related Classifications
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