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D4R antagonis-2
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Catalog No. T62054
D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM) with favorable in vitro pharmacokinetic parameters and good brain penetration, making it a potential research candidate for Parkinson's disease.
D4R antagonis-2
D4R antagonis-2
Copy Product Info😃Good
Catalog No. T62054
D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM) with favorable in vitro pharmacokinetic parameters and good brain penetration, making it a potential research candidate for Parkinson's disease.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 10-14 weeks | 10-14 weeks | |
| 50 mg | $1,980 | 10-14 weeks | 10-14 weeks | |
| 100 mg | $2,500 | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM) with favorable in vitro pharmacokinetic parameters and good brain penetration, making it a potential research candidate for Parkinson's disease. |
| Targets&IC50 | D4 Receptor:6.87 μM |
| In vitro | D4R antagonist-2 (compound 11a) demonstrates significant activity with a K i of 299.4 nM [1]. |
| In vivo | D4R antagonist-2 exhibits highly favorable pharmacokinetic (PK) parameters in vitro and demonstrates significant brain penetration (Kp=2.9) [1]. In rats, administered intravenously at a dose of 0.25 mg/kg, it shows a clearance rate (CL) of 22.0 ml/min/kg, a half-life (T1/2) of 4.4 hours, an initial concentration (C0) of 91 ng/ml, a steady-state volume of distribution (Vss) of 5.5 L/kg, and an area under the curve (AUC) of 747 h*ng/mL [1]. These results underscore D4R antagonist-2's potential for efficacious brain targeting. |
| Molecular Weight | 408.87 |
| Formula | C21H23ClF2N2O2 |
| Smiles | #N/A |
| Storage | Powder: -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:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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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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