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| Cas No.: | 1262132-81-9 |
| Chemical Name: | Enarodustat |
| Synonyms: | JTZ 951;JTZ951;Enarodustat |
| SMILES: | C(O)(=O)CNC(C1=C(O)C=C(CCC2=CC=CC=C2)N2N=CN=C12)=O |
| Formula: | C17H16N4O4 |
| M.Wt: | 340.34 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia. |
| Target: | EC50: 0.22 μM (factor prolyl hydroxylase)[1] |
| In Vivo: | Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats[1]. |
| In Vitro: | Enarodustat (JTZ-951) is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat exhibits neither CYP (IC50 > 100 μM; CYP3A4/5, CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2C8, CYP2B6) nor hERG (IC50 > 100 μM) inhibition[1]. |
| References: | [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. |