FG-2216

Modify Date: 2024-01-09 13:58:59

FG-2216 Structure
FG-2216 structure
Common Name FG-2216
CAS Number 223387-75-5 Molecular Weight 280.66400
Density N/A Boiling Point N/A
Molecular Formula C12H9ClN2O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of FG-2216


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].

 Names

Name [[(1-Chloro-4-hydroxyisoquinolin-3-yl)carbonyl]amino]acetic acid
Synonym More Synonyms

 FG-2216 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
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.

 Chemical & Physical Properties

Molecular Formula C12H9ClN2O4
Molecular Weight 280.66400
Exact Mass 280.02500
PSA 99.52000
LogP 1.79910
Storage condition -20℃

 Synonyms

[(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
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