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CAS No. | 2245053-57-8 | Cat. No. | BCP46430 |
Name | Etavopivat | ||
Synonyms | FT-4202;FT 4202;FT4202; | ||
SMILES | C1COC2=C(O1)C=C(C=N2)S(=O)(=O)N3CC4=C(C3)CN(C4)C(=O)C(CO)C5=CC=CC=C5 | ||
Chemical Name | |||
Formula | C22H23N3O6S | M. Wt | 457.5 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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. |
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