FG2216|cas 223387-75-5|DC Chemicals

Cas No.:	223387-75-5
Chemical Name:	N-[(1-Chloro-4-hydroxyisoquinolin-3-YL)carbonyl]glycine
Synonyms:	Glycine, N-[(1-chloro-4-hydroxy-3-isoquinolinyl)carbonyl]-;FG 2216;FG-2216;YM-311;IOX 3;N-[(1-Chloro-4-hydroxy-3-isoquinolinyl)carbonyl]glycine;YM 311;[[(1-Chloro-4-hydroxyisoquinolin-3-yl)carbonyl]amino]acetic acid;FG 2216 (erythropoietic agent);FG2216;N-[(1-CHLORO-4-HYDROXYISOQUINOLIN-3-YL)CARBONYL]GLYCINE;RU921DS4Z5;2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)acetic acid;UN9;2-[(1-chloro-4-hydroxyisoquinoline-3-carbonyl)amino]acetic acid;Isoquinoline 3;4bqx;OUQVKRKGTAUJQA-UHFFFAOYSA-N;4ie6;2y34;BCP15220;AOB87331;(((1-Chloro-4-hyd
SMILES:	ClC1C2=C([H])C([H])=C([H])C([H])=C2C(=C(C(N([H])C([H])([H])C(=O)O[H])=O)N=1)O[H]
Formula:	C₁₂H₉ClN₂O₄
M.Wt:	280.6639
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].

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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC10339	Vadadustat	Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
DC7486	PX-478 2HCL	PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.
DC10464	PT2385	PT2385 is an orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity.
DC8390	Oltipraz	Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
DC12043	KHS-101	KHS101 is a selective inducer of neuronal differentiation; induces neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50 ~1 μM).
DC8447	KC7F2	KC7F2 is a potent HIF-1 pathway inhibitor and that its potential as a cancer therapy agent warrants further study.
DC8617	JNJ-42041935	JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
DC10825	IOX4	IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).
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DC5193	Roxadustat(FG-4592)	FG-4592 is an HIF αprolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.