nAChR-IN-1
Based on 1 Customer Validation
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.
- Purity: ≥98.0%
- CAS No.: 849461-90-1
- Formula: C16H31NO2
- Molecular Weight:269.42
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nicotine-induced mice model[1]
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Dosage:20 mg/kg
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Administration:Subcutaneous injection; single dose; 15 minutes prior to the injection of nicotine (1.5 mg/kg)
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Result:Increased locomotor activity in mice, even if nicotine-induced decrease.
Showed no effect on body temperature.
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Animal Model:Tail-flick and hot-platemodel in mice[1]
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Dosage:0, 0.1, 1, 5 mg/kg
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Administration:Subcutaneous injection; single dose
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Result:Blocked the antinociceptive effect of nicotine in the hot-plate.
Time-dependently blocked nicotine-induced antinociception.
Chemical Information
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CAS No. 849461-90-1
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Appearance Liquid
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Molecular Weight 269.42
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Formula C16H31NO2
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Color Colorless to light yellow
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SMILES
CCCCCCC(OC1CC(C)(C)NC(C)(C)C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
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)
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.
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.
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 (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.
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.
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 (protect from 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 (270 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 (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 |