Free shipping on all orders over $ 500

FG-2216 (BIQ)

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

YM-311

Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

References

[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

Related HIF Products
Verucopeptin

Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor that reduces the expression of HIF-1 target genes and the protein level of HIF-1α. It is commonly used for cancer-related studies.

TP0463518

TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.

IDF-11774

IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.

HIF-2α-IN-1

HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.

Echinomycin

Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.

  Catalog
Abmole Inhibitor Catalog




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.