N-{(4R)-4-(4-Methoxyphenyl)-3-[2-(4-methoxyphenyl)ethyl]-2-oxo-1- imidazolidinyl}methanesulfonamide

• 常用名: N-{(4R)-4-(4-Methoxyphenyl)-3-[2-(4-methoxyphenyl)ethyl]-2-oxo-1- imidazolidinyl}methanesulfonamide
• 英文名: N-{(4R)-4-(4-Methoxyphenyl)-3-[2-(4-methoxyphenyl)ethyl]-2-oxo-1- imidazolidinyl}methanesulfonamide
• CAS号: 1000306-34-2
• 分子量: 419.49500
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₂₅N₃O₅S
• 熔点: N/A
• 闪点: N/A

用途

KVI-020是心房钾通道Kv1.5的口服活性、强效和选择性阻断剂,IC50为480 nM。KVI-020可以抑制hERG,IC50为15100 nM。KVI-020是一种有效的抗心律失常剂,可用于心房颤动(AF)研究[1]。

名称

• 英文名: N-{(4R)-4-(4-Methoxyphenyl)-3-[2-(4-methoxyphenyl)ethyl]-2-oxo-1- imidazolidinyl}methanesulfonamide

生物活性

• 描述: KVI-020是心房钾通道Kv1.5的口服活性、强效和选择性阻断剂,IC50为480 nM。KVI-020可以抑制hERG,IC50为15100 nM。KVI-020是一种有效的抗心律失常剂,可用于心房颤动(AF)研究[1]。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 靶点实验:

  IC50: 480 ± 44 nM (Kv1.5), 15100 nM (hERG)[1]

• 参考文献:

  [1]. Blass BE, et al. Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia. J Med Chem. 2009 Nov 12;52(21):6531-4.

物理化学性质

• 分子式: C₂₀H₂₅N₃O₅S
• 分子量: 419.49500
• 精确质量: 419.15100
• PSA: 96.56000
• LogP: 3.53690
• InChIKey: GFFIHDXPUGXVGG-IBGZPJMESA-N
• SMILES: COc1ccc(CCN2C(=O)N(NS(C)(=O)=O)CC2c2ccc(OC)cc2)cc1

靶点实验

查看更多实验

实验名称：ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with wh... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301365

实验名称：ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with wh... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301367

实验名称：ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with wh... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301366

实验名称：Selectivity ratio of IC50 for human Kv1.5 to IC50 for human ERG 来源：ChEMBL 靶标：N/A External Id：CHEMBL1039572

实验名称：Metabolic stability in human liver microsomes assessed as half life 来源：ChEMBL 靶标：Liver microsomes External Id：CHEMBL1039570

实验名称：Inhibition of CYP3A4 at 3 uM by fluorescent method 来源：ChEMBL 靶标：Cytochrome P450 3A4 External Id：CHEMBL1039571

实验名称：Aqueous solubility at pH 7.4 by direct UV method 来源：ChEMBL 靶标：N/A External Id：CHEMBL1039569

实验名称：Metabolic stability in Beagle dog liver microsomes assessed as half life 来源：ChEMBL 靶标：N/A External Id：CHEMBL1039586

实验名称：Half life in Beagle dog at 3 mg/kg, iv 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1041423

实验名称：AUC in Beagle dog at 3 mg/kg, iv 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1041424

共32条，当前第1页，共4页

1

2

3

4