产品
编 号：F280670
分子式：C12H9ClN2O4
分子量：280.66
分子式：C12H9ClN2O4
分子量：280.66
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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2mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 223387-75-5
产品详情
生物活性：
FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo.
体内研究：
FG-2216 (40-60 mg/kg; p.o. twice a week for 150 d) induces erythropoiesis and a small elevation of hemoglobin (HbF) expression, and is well tolerated in rhesus macaques.FG-2216 (50 mg/kg; p.o. once daily for 4 or 12 d) increases hematocrit, red blood cell counts, and hemoglobin levels in mice.FG-2216 (40-60 mg/kg; a single p.o) reversibly induces endogenous Epo in rhesus macaques.Animal Model:Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation
Dosage:40, 60 mg/kg
Administration:P.o. (40 mg/kg) twice a week for 6-8 weeksP.o. (60 mg/kg) twice a week for 6-8 weeksP.o. (60 mg/kg) twice a week for 6-8 weeks
Result:Exhibited reticulocytosis within 1-2 weeks of dosing.Increased total hemoglobin levels at the end of the study duration.
体外研究：
FG-2216 (50-100 μM; 24 h) stimulates erythropoietin (Epo) secretion by PHD2 inhibition in Hep3B cells.FG-2216 (3-100 μM; 24 h) stabilizes HIF-1α and HIF-2α in Hep3B cells.
FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo.
体内研究：
FG-2216 (40-60 mg/kg; p.o. twice a week for 150 d) induces erythropoiesis and a small elevation of hemoglobin (HbF) expression, and is well tolerated in rhesus macaques.FG-2216 (50 mg/kg; p.o. once daily for 4 or 12 d) increases hematocrit, red blood cell counts, and hemoglobin levels in mice.FG-2216 (40-60 mg/kg; a single p.o) reversibly induces endogenous Epo in rhesus macaques.Animal Model:Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation
Dosage:40, 60 mg/kg
Administration:P.o. (40 mg/kg) twice a week for 6-8 weeksP.o. (60 mg/kg) twice a week for 6-8 weeksP.o. (60 mg/kg) twice a week for 6-8 weeks
Result:Exhibited reticulocytosis within 1-2 weeks of dosing.Increased total hemoglobin levels at the end of the study duration.
体外研究：
FG-2216 (50-100 μM; 24 h) stimulates erythropoietin (Epo) secretion by PHD2 inhibition in Hep3B cells.FG-2216 (3-100 μM; 24 h) stabilizes HIF-1α and HIF-2α in Hep3B cells.
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