1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. Adiphenine hydrochloride

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.

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Adiphenine hydrochloride Chemical Structure

Adiphenine hydrochloride Chemical Structure

CAS No. : 50-42-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Adiphenine hydrochloride:

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  • Purity & Documentation

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Description

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[1][2][3].

IC50 & Target

IC50: 1.9 µM (α1 nAChR), 1.8 µM (α3β4 nAChR), 3.7 µM (α4β2 nAChR), 6.3 µM (α4β4 nAChR)[1]

In Vitro

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.

In Vivo

Adiphenine (i.p.) prevents the hindleg tonic-extensor component of maximal electroshock seizures (MES), with an ED50 of 62 mg/kg in mice[3].

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

Molecular Weight

347.88

Formula

C20H26ClNO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCN(CC)CC)C(C1=CC=CC=C1)C2=CC=CC=C2.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8746 mL 14.3728 mL 28.7455 mL
5 mM 0.5749 mL 2.8746 mL 5.7491 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 (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.

  • 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

=
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: ≥ 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.
  • Protocol 2

    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.
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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 (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.

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Adiphenine hydrochloride 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.

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Adiphenine hydrochloride
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