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FG-2216

Names

[ CAS No. ]:
223387-75-5

[ Name ]:
FG-2216

[Synonym ]:
[(1-chloro-4-hydroxy-isoquinoline-3-carbonyl)-amino]acetic acid
[(1-chloro-4-hydroxyisoquinoline-3-carbonyl)amino]acetic acid
[(1-Chloro-4-hydroxy-isoquinoline-3-carbonyl)-amino]-acetic acid
(N-(1-chloro-4-hydroxy-isoquinoline-3-carbonyl)-amino)-acetic acid
Glycine, N-[(1-chloro-4-hydroxy-3-isoquinolinyl)carbonyl]-
N-[(1-Chloro-4-hydroxy-3-isoquinolinyl)carbonyl]glycine
N-[(1-chloro-4-hydroxyisoquinolin-3-yl)carbonyl]glycine
FG-2216
[(1chloro-4-hydroxy-isoquinoline-3-carbonyl)amino]-acetic acid
FG2216

Biological Activity

[Description]:

FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.IC50 value: 3.9 uM [1]Target: PDH inhibitorFG-2216 was orally bioavailable and induced significant and reversible Epo induction in vivo (82- to 309-fold at 60 mg/kg). Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry, though significant increases in HbF were not demonstrated by high-pressure liquid chromatography (HPLC) [2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase
Research Areas >> Others

[References]

[1]. Hong YR, et al. [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7.

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


[Related Small Molecules]

Dimethyloxalylglycine | PT-2385 | FG-4592 | PX-478 2HCl | BAY 87-2243 | Vadadustat | Daprodustat | Oltipraz | Chlorogenic acid | LW 6 | Molidustat | IOX2 | Paeoniflorin | KC7F2 | oroxylin A

Chemical & Physical Properties

[ Molecular Formula ]:
C12H9ClN2O4

[ Molecular Weight ]:
280.66400

[ Exact Mass ]:
280.02500

[ PSA ]:
99.52000

[ LogP ]:
1.79910

[ Storage condition ]:
-20℃

Related Compounds