compound introduction
FG-2216 (IOX3) 是一种有效和口服活性的 HIF 脯氨酰羟化酶-2 (PHD2) 抑制剂，IC50 值为 3.9 nM。FG-2216 在体内诱导促红细胞生成素生成和胎儿血红蛋白的表达。 Information FG-2216 FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2 . Phase 2. Targets PHD2 (Cell-free assay) 3.9 μM In vitro FG-2216 shows the ability to stabilize HIF-α to stimulate EPO secretion. In vivo In male rhesus macaques, FG-2216 (60 mg/kg, p.o.), induces significant and reversible Epo induction, and induces a small elevation of HbF expression.
