Etavopivat

  • 化学数据
CAS号 2245053-57-8 货号 BCP46430
中文名 Etavopivat
英文名 Etavopivat
中文别名
英文别名 FT-4202;FT 4202;FT4202;
分子式 C22H23N3O6S 分子量 457.5
  • 用途
生物活性 Etavopivat is an orally available, small-molecule allosteric activator of the selective red blood cell (RBC) isoform of pyruvate kinase (PK-R), with potential to improve symptoms in sickly cell disease (SCD) patients. Upon oral administration, etavopivat allosterically binds to and activates PK-R, thereby enhancing the glycolytic pathway activity in RBCs. This improves adenosine triphosphate (ATP) levels and reduces 2,3-diphosphoglycerate (2,3-DPG) levels in RBCs. This results in increased oxygen affinity, improved RBC deformability, decreased sickle RBC hemolysis, increased hemoglobin (Hb) levels and improved RBC membrane function. Mutations in PK-R cause deficiency in PK-R which prevents adequate RBC glycolysis, leading to a buildup of the upstream glycolytic intermediate 2,3-DPG and deficiency in the PK-R product ATP.
信号通路 Protease/Metabolic Enzyme 
靶 点 Pyruvate Kinase 

结构式

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