TPN171

• 常用名: TPN171
• 英文名: TPN171
• CAS号: 1229018-87-4
• 分子量: 441.57
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₃₅N₅O₃
• 熔点: N/A
• 闪点: N/A

TPN171用途

TPN171 是一种有效选择性的、有口服活性的五型磷酸二酯酶 (PDE5) 抑制剂,IC50 值为 0.62 nM,被开发用于肺动脉高压 (PAH) 的治疗。

TPN171名称

• 中文名: TPN171
• 英文名: TPN171

TPN171生物活性

• 描述: TPN171 是一种有效选择性的、有口服活性的五型磷酸二酯酶 (PDE5) 抑制剂,IC50 值为 0.62 nM,被开发用于肺动脉高压 (PAH) 的治疗。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)
• 靶点实验:

  PDE5:0.62 nM (IC50)

• 参考文献:

  [1]. Wang Z, et al. Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2019 May 23;62(10):4979-4990.

TPN171物理化学性质

• 分子式: C₂₄H₃₅N₅O₃
• 分子量: 441.57

TPN171靶点实验

查看更多实验

实验名称：Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf... 来源：ChEMBL 靶标：cGMP-specific 3',5'-cyclic phosphodiesterase External Id：CHEMBL4397429

实验名称：Terminal half life in human at 5 mg, po administered once daily measured under phase ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4397493

实验名称：Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4397494

实验名称：Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4397430

实验名称：Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in ... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4397495

实验名称：Selectivity ratio of IC50 for N-terminal GST-tagged human PDE6C to IC50 for N-termina... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4397431

实验名称：Metabolic stability in human liver microsomes assessed as parent compound remaining a... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4397432

实验名称：Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-D... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4397497

实验名称：AUC (0 to infinity) in Beagle dog at 0.5 mg/kg, po measured up to 24 hrs by LC-MS/MS ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4397474

实验名称：MRT in Beagle dog at 0.5 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4397475

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