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

NS3861 fumarate 

Cat. No.: HY-110121 Purity: 99.45%
COA Handling Instructions

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.

NS3861 fumarate Chemical Structure

NS3861 fumarate Chemical Structure

CAS No. : 216853-60-0

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NS3861 fumarate:

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Description

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[1].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

400.29

Appearance

Solid

Formula

C16H18BrNO4S
CAS No.
SMILES

BrC1=C(C2=CC(CC3)N(C)C3C2)SC=C1.OC(/C=C/C(O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
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)
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (249.82 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4982 mL 12.4909 mL 24.9819 mL
5 mM 0.4996 mL 2.4982 mL 4.9964 mL
10 mM 0.2498 mL 1.2491 mL 2.4982 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

NS3861216853-60-0NS 3861NS-3861nAChRNicotinic acetylcholine receptorsNicotinic Acetylcholine ReceptorsPatch ClampPharmacologyHeteromericα3β4 nAChRInhibitorinhibitorinhibit

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