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PF-592379

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Catalog No. T10080Cas No. 710655-15-5

PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).

PF-592379

PF-592379

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Catalog No. T10080Cas No. 710655-15-5
PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
25 mg$1,5206-8 weeks6-8 weeks
50 mg$1,9806-8 weeks6-8 weeks
100 mg$2,5006-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Product Introduction

Bioactivity
Description
PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).
Targets&IC50
D3 receptor:(EC50)21 nM
In vitro
PF-592379 is a potent and selective dopamine 3 agonist with an Emax of 95% compared to Pramipexole [1]. It exhibits an EC50 of 21 nM and Ki of 322 nM [2], showing high affinity to human D3 receptors (Ki=215 nM) and a 19-fold selectivity over D4 receptors (Ki=4165 nM). PF-592379 does not bind to D1, human D2, or D5 receptors at concentrations up to 10 μM (Ki≥10 μM) [3].
In vivo
PF-592379 acts as an oral dopamine 3 agonist in rats and dogs. It exhibits a clearance rate of 6.3 and 8.5 mL/min/kg in dogs and 44.8 and 58.2 mL/min/kg in rats, considered low to moderate relative to liver blood flow. The compound demonstrates high permeability in Caco-2 cells and shows complete absorption in pharmacokinetic studies carried out on rats and dogs, achieving oral bioavailability rates of 28% in rats and 61 to 87% in dogs [1].
Chemical Properties
Molecular Weight235.33
FormulaC13H21N3O
Cas No.710655-15-5
SmilesC(CC)N1C[C@H](OC[C@@H]1C)C=2C=CC(N)=NC2
Relative Density.1.058 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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% Saline/PBS/ddH2O

Dose Conversion

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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

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