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Pazinaclone

Name: Pazinaclone
Brand: TargetMol
SKU: T28303
Rating: 4.5 (1 reviews)

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Catalog No. T28303Cas No. 103255-66-9

Alias DN-2327, DN2327, DN 2327, A-77000, A77000, A 77000

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

Pazinaclone

🥰Excellent

Purity: 98.65%

Catalog No. T28303Alias DN-2327, DN2327, DN 2327, A-77000, A77000, A 77000Cas No. 103255-66-9

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

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Purity:98.65%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.
In vivo	Pazinaclone (5 mg/kg; oral; rats, mice, hamsters, and guinea pigs) unchanged drug concentration in plasma was highest in mice (AUC; 90 ng/h/ml), followed in decreasing order by guinea pigs (AUC; 41 ng/h/ml), hamsters (AUC; 18 ng/h/ml), and rats (AUC; 17 ng/h/ml). Among rabbits, dogs, and monkeys, the dogs had the highest plasma drug concentrations: AUCs of pazinaclone in dogs and monkeys were 1035 and 458 ng. h/ml, respectively (drug concentration in rabbit plasma was very low). Of the two polymorphs, forms 1 and 2 with particle size of < or = 5 microns, the oral absorption of form 2 in rats was more efficient than that of form 1 at 1000 mg/kg: AUCs of pazinaclone after dosing of form 1 and 2 were 489 and 965 ng.h/ml, respectively.[2]
Synonyms	DN-2327, DN2327, DN 2327, A-77000, A77000, A 77000

Chemical Properties

Molecular Weight	478.93
Formula	C₂₅H₂₃ClN₄O₄
Cas No.	103255-66-9
Smiles	C(C(=O)N1CCC2(CC1)OCCO2)C3N(C(=O)C=4C3=CC=CC4)C5=NC6=C(C=C5)C=CC(Cl)=N6
Relative Density.	1.48 g/cm3 (Predicted)

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: 4.79 mg/mL (10 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0880 mL	10.4399 mL	20.8799 mL	104.3994 mL
5 mM	0.4176 mL	2.0880 mL	4.1760 mL	20.8799 mL
10 mM	0.2088 mL	1.0440 mL	2.0880 mL	10.4399 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