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    FG-2216 (YM-311; IOX-3; YM-311)
    FG-2216 (YM-311; IOX-3; YM-311)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0298
    CAS #: 223387-75-5Purity ≥98%

    Description: FG-2216 (YM311; IOX3; YM311) is a novel, potent, and orally bioactive inhibitor of hypoxia-inducible factor-1α (HIF) prolyl 4-hydroxylase (PHD) with the potential to treat anemia. It inhibits HIF-PHD with an IC50 of 3.9 μM. 

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

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    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

    IOX3; IOX 3; IOX-3; FG-2216; FG 2216; FG2216; YM311; YM-311; YM 311.


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    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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    FG-2216

    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.

    FG-2216Blood. 2007 Sep 15;110(6):2140-7.

    FG-2216

    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.


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