2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. NS3861

NS3861 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.

NS3861 Chemical Structure

NS3861 Chemical Structure

CAS No. : 216853-59-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 90 In-stock
25 mg USD 210 In-stock
50 mg USD 350 In-stock
100 mg USD 560 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NS3861:

NS3861 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NS3861 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[1].

In Vitro

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[1].
NS3861 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.

NS3861 Related Antibodies
Molecular Weight

284.22

Formula

C12H14BrNS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

BrC1=C(SC=C1)C2=CC(CCC3C2)N3C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (175.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5184 mL 17.5920 mL 35.1840 mL
5 mM 0.7037 mL 3.5184 mL 7.0368 mL
View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.80 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.80 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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 (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.78%

COA (251 KB) HNMR (250 KB) LCMS (93 KB)

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 (protect from 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 3.5184 mL 17.5920 mL 35.1840 mL 87.9600 mL
5 mM 0.7037 mL 3.5184 mL 7.0368 mL 17.5920 mL
10 mM 0.3518 mL 1.7592 mL 3.5184 mL 8.7960 mL
15 mM 0.2346 mL 1.1728 mL 2.3456 mL 5.8640 mL
20 mM 0.1759 mL 0.8796 mL 1.7592 mL 4.3980 mL
25 mM 0.1407 mL 0.7037 mL 1.4074 mL 3.5184 mL
30 mM 0.1173 mL 0.5864 mL 1.1728 mL 2.9320 mL
40 mM 0.0880 mL 0.4398 mL 0.8796 mL 2.1990 mL
50 mM 0.0704 mL 0.3518 mL 0.7037 mL 1.7592 mL
60 mM 0.0586 mL 0.2932 mL 0.5864 mL 1.4660 mL
80 mM 0.0440 mL 0.2199 mL 0.4398 mL 1.0995 mL
100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8796 mL
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NS3861 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NS3861216853-59-7NS 3861NS-3861nAChRNicotinic acetylcholine receptorsNicotinic Acetylcholine ReceptorsPatch ClampPharmacologyHeteromericα3β4 nAChRInhibitorinhibitorinhibit

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