Adiphenine hydrochloride
Based on 3 publication(s) in Google Scholar
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects.
For research use only. We do not sell to patients.
- Purity: 99.14%
- CAS No.: 50-42-0
- Formula: C20H26ClNO2
- Molecular Weight:347.88
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Adiphenine hydrochloride
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Biological Activity
IC50: 1.9 µM (α1 nAChR), 1.8 µM (α3β4 nAChR), 3.7 µM (α4β2 nAChR), 6.3 µM (α4β4 nAChR)[1]
Adiphenine (10 nM-1 mM; 3 min) blocks the function of α1*-nAChR in a dose-dependent manner in TE671/RD cells, with an IC50 of 1.9 μM[1].
Adiphenine (10 nM-1 mM; 3 min) blocks the function of α3α4*-nAChR in a dose-dependent manner in SH-SY5Y cells, with an IC50 of 1.8 μM[1].
Adiphenine (10 nM-1 mM; 3 min) blocks the function of α4β2- and α4β4-nAChR in a dose-dependent manner in SH-EP1 cells, with IC50s of 3.7 and 6.3 μM, respectively[1].
Adiphenine (50-200 μM; 30-60 s) decreases the frequency of ACh-induced single-channel currents in HEK 293 cells[2].
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.
Chemical Information
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CAS No. 50-42-0
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Appearance Solid
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Molecular Weight 347.88
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Formula C20H26ClNO2
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Color White to off-white
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SMILES
O=C(OCCN(CC)CC)C(C1=CC=CC=C1)C2=CC=CC=C2.Cl
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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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Identification of Nicotinic Acetylcholine Receptor for N-Acetylcysteine to Rescue Nicotine-induced Injury Using Beating Cilia in Primary Tissue Derived Airway Organoids. [Abstract]2025 Jan;12(1):e2407054. PMID: 39582278 -
Acta Pharmacol Sin
Ursolic acid derivative UA312 ameliorates ionizing radiation-induced cardiotoxicity and neurodevelopmental toxicity in zebrafish via targeting chrna3 and grik5. [Abstract]2025 Apr 28. PMID: 40295836 -
J Neurochem
Adiphenine Alleviates Impulsive-Like Behaviors in Aged Mice by Inhibiting Nicotinic Acetylcholine Receptors. [Abstract]2025 Aug;169(8):e70190. PMID: 40772705
Solvent & Solubility
DMSO : ≥ 100 mg/mL (287.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (143.73 mM)
* "≥" means soluble, but saturation unknown.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 3.25 mg/mL (9.34 mM); Clear solution
This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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: ≥ 3.25 mg/mL (9.34 mM); Clear solution
This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Gentry CL, et, al. Local anesthetics noncompetitively inhibit function of four distinct nicotinic acetylcholine receptor subtypes. J Pharmacol Exp Ther. 2001 Dec;299(3):1038-48. [Content Brief]
[2]. Spitzmaul, G., et al., The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms. Br J Pharmacol, 2009. 157(5): p. 804-17. [Content Brief]
[3]. TANAKA K, et, al. Anticonvulsant properties of procaine, cocaine, adiphenine and related structures. Proc Soc Exp Biol Med. 1955 Oct;90(1):192-5. [Content Brief]
[4]. Michelot, J., et al., Adiphenine plasma levels and blood-brain barrier crossing in the rat. Eur J Drug Metab Pharmacokinet, 1985. 10(4): p. 273-8. [Content Brief]
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). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.8746 mL | 14.3728 mL | 28.7455 mL | 71.8639 mL |
| 5 mM | 0.5749 mL | 2.8746 mL | 5.7491 mL | 14.3728 mL | |
| 10 mM | 0.2875 mL | 1.4373 mL | 2.8746 mL | 7.1864 mL | |
| 15 mM | 0.1916 mL | 0.9582 mL | 1.9164 mL | 4.7909 mL | |
| 20 mM | 0.1437 mL | 0.7186 mL | 1.4373 mL | 3.5932 mL | |
| 25 mM | 0.1150 mL | 0.5749 mL | 1.1498 mL | 2.8746 mL | |
| 30 mM | 0.0958 mL | 0.4791 mL | 0.9582 mL | 2.3955 mL | |
| 40 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7966 mL | |
| 50 mM | 0.0575 mL | 0.2875 mL | 0.5749 mL | 1.4373 mL | |
| 60 mM | 0.0479 mL | 0.2395 mL | 0.4791 mL | 1.1977 mL | |
| 80 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL | |
| 100 mM | 0.0287 mL | 0.1437 mL | 0.2875 mL | 0.7186 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.