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PF-03463275

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Catalog No. T61564Cas No. 1173239-39-8
Alias PF-3463275

PF-03463275 is an orally active and selective reversible inhibitor of competitive glycine transporter protein-1 (GlyT1) with a Ki of 11.6 nM.PF-03463275 has CNS permeability and may be used to ameliorate cognitive deficits associated with schizophrenia.

PF-03463275

PF-03463275

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Purity: 99.95%
Catalog No. T61564Alias PF-3463275Cas No. 1173239-39-8
PF-03463275 is an orally active and selective reversible inhibitor of competitive glycine transporter protein-1 (GlyT1) with a Ki of 11.6 nM.PF-03463275 has CNS permeability and may be used to ameliorate cognitive deficits associated with schizophrenia.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$51-In Stock
5 mg$122-In Stock
10 mg$197-In Stock
25 mg$333-In Stock
50 mgPreferential-In Stock
1 mL x 10 mM (in DMSO)$133-In 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:99.95%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PF-03463275 is an orally active and selective reversible inhibitor of competitive glycine transporter protein-1 (GlyT1) with a Ki of 11.6 nM.PF-03463275 has CNS permeability and may be used to ameliorate cognitive deficits associated with schizophrenia.
Targets&IC50
GlyT1:11.6 nM(Ki)
In vivo
PF-03463275 (1-10 mg/kg; s.c.; Male Sprague-Dawley rats) induces a dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from dark-adapted rats.[2]
SynonymsPF-3463275
Chemical Properties
Molecular Weight376.86
FormulaC19H22ClFN4O
Cas No.1173239-39-8
Smiles[H][C@@]12CN(C)C[C@]1([H])[C@H]2CN(Cc1ccc(F)c(Cl)c1)C(=O)c1cn(C)cn1
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: 30 mg/mL (79.61 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.65 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 mM2.6535 mL13.2675 mL26.5351 mL132.6753 mL
5 mM0.5307 mL2.6535 mL5.3070 mL26.5351 mL
10 mM0.2654 mL1.3268 mL2.6535 mL13.2675 mL
20 mM0.1327 mL0.6634 mL1.3268 mL6.6338 mL
50 mM0.0531 mL0.2654 mL0.5307 mL2.6535 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% 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

Keywords

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