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FG-2216
- YM 311
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C12H9ClN2O4
- MW: 280.66
Description
Orally active HIF prolyl 4-hydroxylase inhibitor (P4-HI; IC50 value 3.9 μM for PHD2) that increases plasma EPO levels up to 30-fold in hemodialysis (HD) patients, and reduces cardiac remodeling after myocardial infarction in rats independent of a reduction of collagen maturation or altering growth factors.
More Information
| Parent CAS No. | 223387-75-5 |
|---|---|
| Chemical Name | 2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)acetic acid |
| SMILES | C(O)(=O)CNC(C1=C(O)C2=C(C(Cl)=N1)C=CC=C2)=O |
| MFCD | MFCD23136998 |
| 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 |
| CID | 6914666 |
| Short Description | PHD inhibitor |
References
- WM Bernhardt et al. Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD. J Am Soc Nephrol. 2010 Dec;21(12):2151-6.
- S Philipp et al. Stabilization of hypoxia inducible factor rather than modulation of collagen metabolism improves cardiac function after acute myocardial infarction in rats. Eur J Heart Fail. 2006 Jun;8(4):347-54.
- YR Hong 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.
- MM Hsieh 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.
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