Powder: -20°C for 3 years | In solvent: -80°C for 1 year
D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM). D4R antagonist-2 displays favorable in vitro PK parameters and exhibits good brain penetration. D4R antagonist-2 has the research potential in Parkinson’s disease.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM). D4R antagonist-2 displays favorable in vitro PK parameters and exhibits good brain penetration. D4R antagonist-2 has the research potential in Parkinson’s disease. |
In vitro | D4R antagonist-2 (compound 11a) shows good activity with an 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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D4R antagonis-2 inhibitor inhibit