Molecular Weight (MW)

280.66

Formula

C12H9ClN2O4

CAS No.

223387-75-5

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 56 mg/mL (199.5 mM)

Water:<1 mg/mL

Ethanol:<1 mg/mL

Solubility (In vivo)

Chemical Name: (1-chloro-4-hydroxyisoquinoline-3-carbonyl)glycine

InChi Key: OUQVKRKGTAUJQA-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17)

SMILES Code: OC1=C(C(NCC(O)=O)=O)N=C(Cl)C2=CC=CC=C21

Synonyms

In Vitro

In vitro activity: FG-2216 (IOX3; YM311) 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.

Cell Assay: FG-2216 showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count

In Vivo

In male rhesus macaques, FG-2216 (60 mg/kg, p.o.), induces significant and reversible Epo induction, and induces a small elevation of HbF expression.

Animal model

Male rhesus macaques

Formulation & Dosage

Suspended in 0.5% carboxymethylcellulose (CMC); 60 mg/kg; p.o.

References

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7; Blood. 2007 Sep 15;110(6):2140-7.

Epo-induction in rhesus macques. (A) Circulating plasma Epo levels after a single oral dose of FG-2216. Blood. 2007 Sep 15;110(6):2140-7.

Blood. 2007 Sep 15;110(6):2140-7.

Hemoglobin increases by PHI. (A) Hemoglobin (g/dL) values are presented with respect to number of days on treatment in 1 rhesus macaque treated with FG-2216 (●) and 1 control animal (○). (B) Hemoglobin levels in treated and control rhesus macaques. Blood.2007 Sep 15;110(6):2140-7.