CAS 223387-75-5|FG-2216

Introduction：Basic information about CAS 223387-75-5|FG-2216, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. FG-2216 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

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

Names

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

FG-2216 BiologicalActivity

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-HydroxylaseResearch 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.

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-HydroxylaseResearch 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.

Chemical & Physical Properties

Molecular Formula	C₁₂H₉ClN₂O₄
Molecular Weight	280.66400
Exact Mass	280.02500
PSA	99.52000
LogP	1.79910
InChIKey	OUQVKRKGTAUJQA-UHFFFAOYSA-N
SMILES	O=C(O)CNC(=O)c1nc(Cl)c2ccccc2c1O
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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