223387-75-5

223387-75-5 structure

Name: FG-2216
Chemical Name: [[(1-Chloro-4-hydroxyisoquinolin-3-yl)carbonyl]amino]acetic acid
CAS Number: 223387-75-5
Molecular Formula: C₁₂H₉ClN₂O₄
Molecular Weight: 280.66400
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2019-02-17 10:24:55
Modify Date: 2024-01-09 13:58:59
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].

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

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.