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Mardepodect

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Catalog No. T16499Cas No. 898562-94-2
Alias PF-2545920

Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM and over 1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier.

Mardepodect

Mardepodect

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Purity: 99.94%
Catalog No. T16499Alias PF-2545920Cas No. 898562-94-2
Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM and over 1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$36In StockIn Stock
5 mg$84In StockIn Stock
10 mg$153In StockIn Stock
25 mg$247In StockIn Stock
50 mg$385In StockIn Stock
100 mg$576In StockIn Stock
200 mg$825In StockIn Stock
1 mL x 10 mM (in DMSO)$93In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.94%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM and over 1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier.
Targets&IC50
PDE10A:0.37 nM
In vivo
Mardepodect is active in a range of antipsychotic models with the ED50 of 1 mg/kg, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.Mardepodect induces a dose-dependent increase in striatal cGMP in mice.
SynonymsPF-2545920
Chemical Properties
Molecular Weight392.45
FormulaC25H20N4O
Cas No.898562-94-2
SmilesCn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (114.66 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.1 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5481 mL12.7405 mL25.4810 mL127.4048 mL
5 mM0.5096 mL2.5481 mL5.0962 mL25.4810 mL
10 mM0.2548 mL1.2740 mL2.5481 mL12.7405 mL
20 mM0.1274 mL0.6370 mL1.2740 mL6.3702 mL
50 mM0.0510 mL0.2548 mL0.5096 mL2.5481 mL
100 mM0.0255 mL0.1274 mL0.2548 mL1.2740 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:
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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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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