AZD5462

• 常用名: AZD5462
• 英文名: AZD5462
• CAS号: 2787501-83-9
• 分子量: 544.65
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₀H₄₁FN₂O₆
• 熔点: N/A
• 闪点: N/A

AZD5462用途

AZD5462是一种RXFP1调制器,可用于心力衰竭研究。RXFP1是人类松弛素的同源受体,属于GPCR家族1c号,具有抗纤维化和抗炎特性[1]。

AZD5462名称

• 英文名: AZD5462

AZD5462生物活性

• 描述: AZD5462是一种RXFP1调制器,可用于心力衰竭研究。RXFP1是人类松弛素的同源受体,属于GPCR家族1c号,具有抗纤维化和抗炎特性[1]。
• 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:

  RXFP1[1]

• 体外研究: AZD5462(示例1)显示了EC50分别为17 nM和50 nM时对cAMP或cGMP生产的刺激活性[1]。AZD5462结合人血浆蛋白,未结合(游离)率为4.3%,Clint值为23μL/min/mg(人虱微粒体)、4.8μL/min/106细胞(人肝细胞)和11μL/min/106细胞(大鼠肝细胞)时表现出稳定性[1]。AZD5462以6.3 nM的EC50值增强ERK的磷酸化[1]。
• 参考文献:

  [1]. Granberg Kenneth Lars, et al. 4-(2-Fluoro-4-methoxy-5-(3-(((1-methylcyclobutyl)methyl)carbamoyl)bicyclo[2.2.1]heptan-2-yl)carbamoyl)phenoxy)-1-methylcyclohexane-1-carboxylic acid derivatives and similar compounds as RXFP1 modulators for the treatment of heart failure and their preparation: World Intellectual Property Organization, WO2022122773. 2022-06-16.

AZD5462物理化学性质

• 分子式: C₃₀H₄₁FN₂O₆
• 分子量: 544.65

AZD5462靶点实验

查看更多实验

实验名称：Volume of distribution at steady state in Han Wistar rat at 0.92 micromol/kg, iv by L... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5522504

实验名称：Metabolic stability in rat hepatocytes assessed as unbound intrinsic clearance measur... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5522502

实验名称：Agonist activity at mouse RXFP1 expressed in CHO-K1 cells assessed as maximal increas... 来源：ChEMBL 靶标：Relaxin receptor 1 External Id：CHEMBL5522501

实验名称：Agonist activity at rat RXFP1 expressed in CHO-K1 cells assessed as maximal increase ... 来源：ChEMBL 靶标：Relaxin receptor 1 External Id：CHEMBL5522499

实验名称：Metabolic stability in human liver microsomes assessed as unbound intrinsic clearance... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5522497

实验名称：Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5522496

实验名称：Metabolic stability in human hepatocytes assessed as unbound intrinsic clearance meas... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5522495

实验名称：Metabolic stability in human hepatocytes assessed as intrinsic clearance measured per... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5522494

实验名称：Agonist activity at human RXFP1 expressed in CHO cells assessed as maximal increase i... 来源：ChEMBL 靶标：Relaxin receptor 1 External Id：CHEMBL5522492

实验名称：Agonist activity at human RXFP1 expressed in CHO cells assessed as increase in cAMP l... 来源：ChEMBL 靶标：Relaxin receptor 1 External Id：CHEMBL5522491

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