Identification | Back Directory | [Name]
FG 2216 | [CAS]
223387-75-5 | [Synonyms]
BIQ FG2216 YM 311 FG-2216 FG 2216 CS-1687 FG-2216(IOX3 FG-2216 - YM 311 FG2216;FG-2216;FG 2216 FG 2216 (erythropoietic agent) N-[(1-Chloro-4-hydroxy-3-isoquinolinyl)carbonyl]glycine Glycine, N-[(1-chloro-4-hydroxy-3-isoquinolinyl)carbonyl]- 2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)acetic acid [[(1-Chloro-4-hydroxyisoquinolin-3-yl)carbonyl]amino]acetic acid (N-(1-chloro-4-hydroxy-isoquinoline-3-carbonyl)-amino)-acetic acid (Z)-2-(((1-CHLORO-4-HYDROXYISOQUINOLIN-3-YL)(HYDROXY)METHYLENE)AMINO)ACETIC ACID | [Molecular Formula]
C12H9ClN2O4 | [MOL File]
223387-75-5.mol | [Molecular Weight]
280.66 |
Chemical Properties | Back Directory | [Boiling point ]
670.6±55.0 °C(Predicted) | [density ]
1.571±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
insoluble in H2O; ≥14.05 mg/mL in DMSO; ≥5.12 mg/mL in EtOH with ultrasonic | [form ]
powder | [pka]
3.20±0.10(Predicted) | [color ]
white to beige |
Hazard Information | Back Directory | [Description]
FG-2216 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC50 = 3.9 micromolar). It has been shown to reversibly stimulate erythropoietin secretion at 100 μM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice. | [Uses]
FG 2216 is an erythropoietic agent which is orally active prolyl-hydroxylase inhibitor which increases erythropoietin production in end-stage kidney disease. | [Biochem/physiol Actions]
BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD). BIQ induces significant and reversible plasma erythropoietin (EPO) levels in vitro and in hemodialysis patients. | [References]
1. hsieh mm, linde ns, wynter a et al. hif prolyl hydroxylase inhibitionresults in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. blood. 2007 sep 15;110(6):2140-7. |
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