FG-2216

• CAT Number: I002713
• CAS Number: 223387-75-5
• Molecular Formula: C12H9ClN2O4
• Molecular Weight: 280.7
• Purity: ≥95%
• Target: PDH inhibitor
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: -20°C
• IC50: 3.9 uM
• IUPAC Name: 2-[(1-chloro-4-hydroxyisoquinoline-3-carbonyl)amino]acetic acid
• InChI: 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)
• InChIKey: OUQVKRKGTAUJQA-UHFFFAOYSA-N
• SMILES: C1=CC=C2C(=C1)C(=C(N=C2Cl)C(=O)NCC(=O)O)O

FG-2216（Cat No.:I002713） is a powerful inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase, with an IC50 of 3.9 uM for the PDH2 enzyme. It is orally bioavailable, meaning it can be administered through the mouth, and has demonstrated significant and reversible induction of erythropoietin (Epo) in vivo. By inhibiting HIF prolyl hydroxylase, FG-2216 stabilizes HIF-α subunits, leading to increased Epo production.

Reference

[1]. Hong YR, et al. [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7.
[2]. Hsieh MM, et al. HIF prolyl hydroxylase inhibition results in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. Blood. 2007 Sep 15;110(6):2140-7.