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

D4R antagonist-2 是一种有效的选择性 D4R 拮抗剂,IC50 为 6.87 µM。 D4R antagonist-2 显示非常有利的体外 PK 参数并且具有较好的脑渗透性。 D4R antagonist-2 具有帕金森病研究潜力。

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D4R antagonis-2 Chemical Structure

D4R antagonis-2 Chemical Structure

CAS No. : 2846077-70-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(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.

体内研究
(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).
分子量

408.87

Formula

C21H23ClF2N2O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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D4R antagonis-2
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HY-145906
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