223387-75-5

Usage

Uses

FG 2216 is an erythropoietic agent which is orally active prolyl-hydroxylase inhibitor which increases erythropoietin production in end-stage kidney disease.

Biochem/physiol Actions

BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD). BIQ induces significant and reversible plasma erythropoietin (EPO) levels in vitro and in hemodialysis patients.

references

1. hsieh mm, linde ns, wynter a et al. hif prolyl hydroxylase inhibitionresults in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. blood. 2007 sep 15;110(6):2140-7.

Upstream product

• 223388-22-5 N-((1-Chloro-4-hydroxyisoquinolin-3-yl)carbonyl)glycine methyl ester 
• 223388-21-4 1-chloro-4-hydroxyisoquinoline-3-carboxylic acid 
• 616-34-2 methoxycarbonylmethylamine 
• 223388-20-3 methyl 1-chloro-4-hydroxyisoquinoline-3-carboxylate 

Relevant academic research and scientific papers

Using NMR solvent water relaxation to investigate metalloenzyme - Ligand binding interactions

This report demonstrates that solvent water relaxation measurements can be used for quantitative screening of ligand binding and for mechanistic investigations of enzymes containing paramagnetic metal centers by using conventional NMR instrumentation at high field. The method was exemplified using prolyl hydroxylase domain containing enzyme 2 (PHD2), a human enzyme involved in hypoxic sensing, with Mn(II) substituting for Fe(II) at the active site. KD values were determined for inhibitors that hinder access of water to the paramagnetic center. This technique is also useful for investigating the mechanism of suitable metalloenzymes, including order of ligand binding and modes of inhibition. 2009 American Chemical Society.

CHEMICAL COMPOUNDS

A compound which is a pyridine or isoquinoline derivative of formula (I), or a pharmaceutically acceptable salt thereof, which is useful in the inhibition of γ- butyrobetaine hydroxylase (BBOX). The compounds are particularly useful in treatment of cardio

Substituted isoquinoline-3-carboxamides, their preparation and their use as pharmaceuticals

Novel isoquinoline-3-carboxamides of the formula I: in which R1 is hydrogen or chlorine, R2 is hydrogen, alkyl, alkoxy, chlorine, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the formula O-[CH2]x-CfH(2f+1-g)Fg, where x=0 or 1, f=1-5, and g=1 to (2f+1), R3 is hydrogen, alkyl, alkoxy, fluorine, chlorine, cyano, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the above formula, R4 and R5 are hydrogen, alkyl, fluorine, chlorine, bromine, trifluoromethyl, cyano, alkoxy, or fluoroalkoxy of the above formula, including the physiologically active salts, are strong prolyl-4-hydroxylase inhibitors which do not cause steatosis.