Enarodustat

Enarodustat is a pan hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor (Kis = 16, 61, and 101 nM for HIF-PH1, -2, and -3, respectively). It increases erythropoietin (EPO) levels in Hep3B cells (EC50 = 4.7 µM). Enarodustat (3 mg/kg) increases plasma EPO levels in control rats, as well as plasma EPO and hemoglobin levels in 5/6-nephrectomized rats. It also decreases renal fatty acid and amino acid metabolism and increases renal glucose metabolism in streptozotocin-induced rat and alloxan-induced mouse models of diabetic nephropathy.Formal Name: N-[[7-hydroxy-5-(2-phenylethyl)[1,2,4]triazolo[1,5-a]pyridin-8-yl]carbonyl]-glycine. CAS Number: 1262132-81-9. Synonyms: JTZ-951. Molecular Formula: C17H16N4O4. Formula Weight: 340.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 224 nm. SMILES: O=C(CNC(C1=C(C=C(CCC2=CC=CC=C2)N3N=CN=C13)O)=O)O. InChi Code: 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/h1-5,8,10,22H,6-7,9H2,(H,18,25)(H,23,24). InChi Key: NALAUGMPMIVAOW-UHFFFAOYSA-N.