1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. mAChR Sodium Channel
  3. Diphenidol hydrochloride

Diphenidol hydrochloride  (Synonyms: Difenidol hydrochloride)

Cat. No.: HY-A0082 Purity: 99.95%
COA Handling Instructions

Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea.

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

Diphenidol hydrochloride Chemical Structure

Diphenidol hydrochloride Chemical Structure

CAS No. : 3254-89-5

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Diphenidol hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea[1][2][3][4][5].

IC50 & Target

mAChR3

 

mAChR2

 

mAChR1

 

mAChR4

 

In Vitro

Diphenidol hydrochloride inhibits sodium currents and produces spinal anesthesia, and at -70 and -100 mV holding potentials, N2A cells IC50 were 0.77 and 62.6 μM, respectively [3].

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

In Vivo

Diphenidol hydrochloride (2, 10 μmoL/kg, intraperitoneal injection) is used to reduce neuropathic pain and TNF-α overexpression in rats after chronic systolic injury[4].
Diphenidol hydrochloride (30 mg/kg, injected intravenously) has an inhibitory effect on exercise and morphine-induced vomiting in pica rats[5].

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

Animal Model: Chronic constriction injury (CCI) rat model[4]
Dosage: 2, 10 μmoL/kg
Administration: i.p., berore surgery, and on postoperative days 3, 6, 7, 11, 13 and 14.
Result: Increased mechanical withdrawal threshold in a dose-dependent manner and decreased the TNF-α level.
Molecular Weight

345.91

Formula

C21H28ClNO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C1=CC=CC=C1)(C2=CC=CC=C2)CCCN3CCCCC3.[H]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 : ≥ 46 mg/mL (132.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 16.67 mg/mL (48.19 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8909 mL 14.4546 mL 28.9093 mL
5 mM 0.5782 mL 2.8909 mL 5.7819 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (7.23 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 (7.23 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.
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 2.8909 mL 14.4546 mL 28.9093 mL 72.2731 mL
5 mM 0.5782 mL 2.8909 mL 5.7819 mL 14.4546 mL
10 mM 0.2891 mL 1.4455 mL 2.8909 mL 7.2273 mL
15 mM 0.1927 mL 0.9636 mL 1.9273 mL 4.8182 mL
20 mM 0.1445 mL 0.7227 mL 1.4455 mL 3.6137 mL
25 mM 0.1156 mL 0.5782 mL 1.1564 mL 2.8909 mL
30 mM 0.0964 mL 0.4818 mL 0.9636 mL 2.4091 mL
40 mM 0.0723 mL 0.3614 mL 0.7227 mL 1.8068 mL
DMSO 50 mM 0.0578 mL 0.2891 mL 0.5782 mL 1.4455 mL
60 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2046 mL
80 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.9034 mL
100 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 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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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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Diphenidol hydrochloride
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