1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. D4R antagonis-2

D4R antagonis-2 

Cat. No.: HY-145906
Handling Instructions

D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease.

For research use only. We do not sell to patients.

D4R antagonis-2 Chemical Structure

D4R antagonis-2 Chemical Structure

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Description

D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease[1].

IC50 & Target

D4 Receptor

6.87 μM (IC50)

In Vitro

D4R antagonist-2 (compound 11a) shows good activity with an Ki of 299.4 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

D4R antagonist-2 displays very favorable in vitro PK parameters and is brain pentrent (Kp=2.9)[1]. b>Pharmacokinetic Parameters of D4R antagonist-2 in rats[1].

rat cassette (0.25 mpk) 11a
CL (ml/min/kg) 22.0
T1/2 (h) 4.4
C0 (ng/ml) 91
Vss (L/kg) 5.5
AUC (h*ng/mL) 747

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: rats[1]
Dosage:
Administration: i.v.
Result: Displayed very favorable in vitro PK parameters and was brain pentrent (Kp=2.9).
Molecular Weight

408.87

Formula

C21H23ClF2N2O2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
D4R antagonis-2
Cat. No.:
HY-145906
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