Enarodustat

• CAT Number: I019938
• CAS Number: 1262132-81-9
• Molecular Formula: C₁₇H₁₆N₄O₄
• Molecular Weight: 340.33
• Purity: ≥95%
• Target: HIF/HIF Prolyl-Hydroxylase
• Storage: Store at -20°C
• IUPAC Name: 2-[[7-oxo-5-(2-phenylethyl)-3H-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl]amino]acetic acid
• InChI: InChI=1S/C17H16N4O4/c22-13-8-12(7-6-11-4-2-1-3-5-11)21-16(19-10-20-21)15(13)17(25)18-9-14(23)24/h1-5,8,10H,6-7,9H2,(H,18,25)(H,19,20)(H,23,24)
• InChIKey: FJYRBJKWDXVHHO-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O

Enarodustat (Cat No.:I019938) is a potent oral inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase. It selectively inhibits PHD2 (prolyl hydroxylase domain 2), resulting in the stabilization of HIF and subsequent upregulation of erythropoietin (EPO) production. Enarodustat has demonstrated an IC50 of 0.22 μM for PHD2 inhibition and an EC50 of 5.7 μM for EPO release from Hep3B cells. With its ability to regulate erythropoiesis, enarodustat shows potential in the treatment of renal anemia, particularly in patients with chronic kidney disease.

Reference

[1]. Ogoshi Y, et al. Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. ACS Med Chem Lett. 2017 Nov 20;8(12):1320-1325.