| 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. | [in vivo]
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[2].
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[1].
FG-2216 (40-60 mg/kg; a single p.o) reversibly induces endogenous Epo in rhesus macaques[2]. | Animal Model: | Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation[2] | | Dosage: | 40, 60 mg/kg | | Administration: | P.o. (40 mg/kg) twice a week for 6-8 weeks
P.o. (60 mg/kg) twice a week for 6-8 weeks
P.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.
|
| [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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