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Biological Activity:

FG-4592 (Roxadustat) is a potent, selective and bioavailable inhibitor of hypoxia-inducible factor prolyl hydroxylase. It is an analog of 2-oxoglutarate (2-OG) to inhibit HIF-PH and prevent HIF turnover. While little has been published regarding the actions of this compound, similar HIF-PH inhibitors suppress HIF degradation and in this way induce erythropoietin expression, promoting erythropoiesis or preventing anemia in vivo. Right now FG-4592 is in phase III clinical trials to treat anemia.

How to Use:

In vitro: FG-4592 was usually used at 10 µM final concentration in vitro.
In vivo: n/a

Reference:

• 1. Hsieh MM, et al. HIF prolyl hydroxylase inhibition results in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. (2007) Blood. 15;110(6):2140-7.