Etavopivat
| 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 |
| 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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