GRK2-IN-1

• 常用名: GRK2-IN-1
• 英文名: GRK2-IN-1
• CAS号: 2055990-90-2
• 分子量: 452.48
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₅FN₄O₄
• 熔点: N/A
• 闪点: N/A

GRK2-IN-1用途

GRKs-IN-1,化合物14as,对G 蛋白偶联受体激酶 2 GRK2 具有显着的效力和选择性 (IC50=30 nM) 和 GRK5 (IC50=7.1 μM)。GRKs-IN-1 是帕罗西汀的衍生物,与帕罗西汀相比,心肌细胞收缩性测定显示改善了 100 倍。

GRK2-IN-1名称

• 英文名: GRK2-IN-1

GRK2-IN-1生物活性

• 描述: GRKs-IN-1,化合物14as,对G 蛋白偶联受体激酶 2 GRK2 具有显着的效力和选择性 (IC50=30 nM) 和 GRK5 (IC50=7.1 μM)。GRKs-IN-1 是帕罗西汀的衍生物,与帕罗西汀相比,心肌细胞收缩性测定显示改善了 100 倍。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 其他 >> 其他
• 靶点实验:

  GRK2:30 nM (IC50)

  GRK5:7.1 μM (IC50)

• 参考文献:

  [1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.

GRK2-IN-1物理化学性质

• 分子式: C₂₄H₂₅FN₄O₄
• 分子量: 452.48

GRK2-IN-1靶点实验

查看更多实验

实验名称：Half life in CD-1 mouse liver microsomes at 1 uM measured up to 60 mins in presence o... 来源：ChEMBL 靶标：Liver External Id：CHEMBL4043643

实验名称：Selectivity ratio of IC50 for mouse PKA to IC50 for bovine GRK2 来源：ChEMBL 靶标：N/A External Id：CHEMBL4043641

实验名称：Selectivity index, ratio of IC50 for ROCK1 (unknown origin) to IC50 for bovine GRK2 来源：ChEMBL 靶标：N/A External Id：CHEMBL4043642

实验名称：Selectivity ratio of IC50 for bovine GRK5 to IC50 for bovine GRK2 来源：ChEMBL 靶标：N/A External Id：CHEMBL4043639

实验名称：Selectivity ratio of IC50 for bovine GRK1 to IC50 for bovine GRK2 来源：ChEMBL 靶标：N/A External Id：CHEMBL4043640

实验名称：Time at which plasma concentration stays above in vitro bovine GRk2 IC50 in CD-1 mous... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4043653

实验名称：AUC (0 to 7 hrs) in CD-1 mouse at 10 mg/kg, ip administered as single dose by LC-MS/M... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4043652

实验名称：Inhibition of GRK2 in isoproterenol-stimulated C57/BL6 mouse cardiomyocytes assessed ... 来源：ChEMBL 靶标：Beta-adrenergic receptor kinase 1 External Id：CHEMBL4043647

实验名称：Inhibition of mouse PKA using CREBtide as substrate after 30 mins in presence of ATP ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4043637

实验名称：Inhibition of ROCK1 (unknown origin) at 10 uM by ADP-Glo kinase assay 来源：ChEMBL 靶标：Rho-associated protein kinase 1 External Id：CHEMBL4043638

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