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Pipequaline

Name: Pipequaline
Brand: TargetMol
SKU: T4655
Rating: 4.5 (1 reviews)

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Catalog No. T4655Cas No. 77472-98-1

Alias PK-8165

Pipequaline (PK-8165) is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic.

Pipequaline

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Catalog No. T4655Alias PK-8165Cas No. 77472-98-1

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Product Introduction

Bioactivity

Description	Pipequaline (PK-8165) is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic.
In vitro	Pipequaline is extensively bound to plasma proteins: i.e. human serum albumin (HSA), alpha-1-acid glycoprotein (AAG), lipoproteins and blood cells, mainly erythrocytes[1].
In vivo	Intravenously administered pipequaline partially suppresses activations by kainate, glutamate, and acetylcholine. Microiontophoretic applications of pipequaline reduce neuronal activation by kainate[2]. In small intravenous doses, pipequaline potentiates the effect of microiontophoretically-applied flurazepam, whereas in larger doses, it suppresses the effects of microiontophoretically-applied flurazepam and intravenously administered lorazepam on kainate-induced activation. Pipequaline produces dose-related decreases in motor activity and significant dose-related decreases in the number of head-dips made[3].
Animal Research	Rats: Pipequaline is dissolved in water to give injection volumes of 2 mL/kg. Rats are injected with 5, 10, and 50 mg/kg pipequaline. Infrared cells in the walls of the box provided automated measures of locomotor activity and rearing, respectively[3].
Synonyms	PK-8165

Chemical Properties

Molecular Weight	316.44
Formula	C₂₂H₂₄N₂
Cas No.	77472-98-1
Smiles	C(Cc1cc(nc2ccccc12)-c1ccccc1)C1CCNCC1
Relative Density.	1.078g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 32 mg/mL (101.13 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1602 mL	15.8008 mL	31.6016 mL	158.0078 mL
5 mM	0.6320 mL	3.1602 mL	6.3203 mL	31.6016 mL
10 mM	0.3160 mL	1.5801 mL	3.1602 mL	15.8008 mL
20 mM	0.1580 mL	0.7900 mL	1.5801 mL	7.9004 mL
50 mM	0.0632 mL	0.3160 mL	0.6320 mL	3.1602 mL
100 mM	0.0316 mL	0.1580 mL	0.3160 mL	1.5801 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc