GBT-440

GBT-440

CAT N°: 23933
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From 85.00 72.25

GBT-440 is a modulator of sickle hemoglobin (HbS) that binds covalently to the N-terminal valine of the ? chain of HbS.{41378} In vitro, GBT-440 increases HbS affinity for oxygen (EC50s = 8.2 and 415 ?M for purified HbS and whole blood from sickle cell anemia patients, respectively) and delays oxygen release from and polymerization of HbS in a concentration-dependent manner. GBT-440 (100-150 mg/kg) increases red blood cell half-life and reduces sickling ex vivo in whole blood isolated from a murine model of sickle cell anemia. It also reduces ex vivo sickling of sickle cell trait red blood cells under conditions of hypoxia, acidosis, and dehydration.{41379}

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