2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. nAChR-IN-1

nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research.

For research use only. We do not sell to patients.

nAChR-IN-1 Chemical Structure

nAChR-IN-1 Chemical Structure

CAS No. : 849461-90-1

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5 mg USD 110 In-stock
10 mg USD 165 In-stock
25 mg USD 290 In-stock
50 mg USD 460 In-stock
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Based on 1 publication(s) in Google Scholar

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nAChR-IN-1 Related Antibodies

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Description

nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research[1].

In Vitro

nAChR-IN-1 (100 nM) inhibits nAChR with inhibition rate of 90% in Xenovus oocytes, and suppresses AChR subtypes (mouse muscle-type (α1β1εδ) nAChR, three different pairwise combinations of rat neuronal alpha and beta subunits (α3β4, α4β2, and α3β2), and α7 homomeric neuronal nAChR) with IC50s (area) of 390, 1.2, 110, 75, 440, 460, 430, 2.7, 1.0, 1.4, and 18.3 nM, respectively, based on the decrease in the net charge of the ACh response[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

nAChR-IN-1 Related Antibodies
In Vivo

nAChR-IN-1 (20 mg/kg; s.c.; single dose) improves nicotine-induced hypomotility and hypothermia in a time-dependent manner in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nicotine-induced mice model[1]
Dosage: 20 mg/kg
Administration: Subcutaneous injection; single dose; 15 minutes prior to the injection of nicotine (1.5 mg/kg) 
Result: Increased locomotor activity in mice, even if nicotine-induced decrease.
Showed no effect on body temperature.
Animal Model: Tail-flick and hot-platemodel in mice[1]
Dosage: 0, 0.1, 1, 5 mg/kg
Administration: Subcutaneous injection; single dose
Result: Blocked the antinociceptive effect of nicotine in the hot-plate.
Time-dependently blocked nicotine-induced antinociception.
Molecular Weight

269.42

Formula

C16H31NO2
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

CCCCCCC(OC1CC(C)(C)NC(C)(C)C1)=O
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 : 100 mg/mL (371.17 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 3.7117 mL 18.5584 mL 37.1168 mL
5 mM 0.7423 mL 3.7117 mL 7.4234 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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 (9.28 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 (9.28 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
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 3.7117 mL 18.5584 mL 37.1168 mL 92.7919 mL
5 mM 0.7423 mL 3.7117 mL 7.4234 mL 18.5584 mL
10 mM 0.3712 mL 1.8558 mL 3.7117 mL 9.2792 mL
15 mM 0.2474 mL 1.2372 mL 2.4745 mL 6.1861 mL
20 mM 0.1856 mL 0.9279 mL 1.8558 mL 4.6396 mL
25 mM 0.1485 mL 0.7423 mL 1.4847 mL 3.7117 mL
30 mM 0.1237 mL 0.6186 mL 1.2372 mL 3.0931 mL
40 mM 0.0928 mL 0.4640 mL 0.9279 mL 2.3198 mL
50 mM 0.0742 mL 0.3712 mL 0.7423 mL 1.8558 mL
60 mM 0.0619 mL 0.3093 mL 0.6186 mL 1.5465 mL
80 mM 0.0464 mL 0.2320 mL 0.4640 mL 1.1599 mL
100 mM 0.0371 mL 0.1856 mL 0.3712 mL 0.9279 mL
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nAChR-IN-1 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:

nAChR-IN-1849461-90-1nAChRNicotinic acetylcholine receptorsselective inhibitiontetramethylpiperidinyl heptanoateneurol disorderTMPHnicotinic receptordysfunctionneuronal nicotinic receptorsbrain functionInhibitorinhibitorinhibit

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