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

Adiphenine hydrochloride 

Cat. No.: HY-B0379A Purity: 99.77%
Handling Instructions

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 narcotic and anticonvulsant effects.

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

Adiphenine hydrochloride Chemical Structure

Adiphenine hydrochloride Chemical Structure

CAS No. : 50-42-0

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10 mM * 1 mL in DMSO USD 79 In-stock
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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 narcotic and 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].

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].

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

Molecular Weight

347.88

Formula

C₂₀H₂₆ClNO₂

CAS No.

50-42-0

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (287.46 mM)

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
10 mM 0.2875 mL 1.4373 mL 2.8746 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: ≥ 3.25 mg/mL (9.34 mM); Clear solution

  • 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

  • 3.

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

    Solubility: ≥ 3.25 mg/mL (9.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AdipheninenAChRNicotinic acetylcholine receptorsnicotinicacetylcholinelocalanestheticInhibitorinhibitorinhibit

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Adiphenine hydrochloride
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HY-B0379A
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