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FG-2216 (BIQ)

Cat. No. M8678
FG-2216 (BIQ) Structure


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Biological Activity

BIQ (FG-2216) is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme. FG-2216 is orally bioavailable and induced significant and reversible Epo induction 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.

Chemical Information
Molecular Weight 280.66
Formula C12H9ClN2O4
CAS Number 223387-75-5
Solubility (25°C) DMSO: ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Liesl K Janssens, et al. Sensing an Oxygen Sensor: Development and Application of Activity-Based Assays Directly Monitoring HIF Heterodimerization

[2] Pierre E Signore, et al. A small-molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase improves obesity, nephropathy and cardiomyopathy in obese ZSF1 rats

[3] Julia Gnter, et al. Inhibition of firefly luciferase activity by a HIF prolyl hydroxylase inhibitor

[4] Simon Beuck, et al. Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis

[5] Wanja M Bernhardt, et al. Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD

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Abmole Inhibitor Catalog

Keywords: FG-2216 (BIQ), YM-311 supplier, HIF, inhibitors, activators

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