product name FG-2216
Description: FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. FG-2216, also known as YM311, is orally bioavailable and can induce significant and reversible Epo induction in vivo. 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, and hemoglobin levels in an animal efficacy study.
References: Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7; Blood. 2007 Sep 15;110(6):2140-7.
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)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426665
| In Vitro |
In vitro activity: FG-2216 shows the ability to stabilize HIF-α to stimulate EPO secretion. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
