Enarodustat是一种有效的，可口服的factorprolylhydroxylase抑制剂，EC50of0.22μM；Enarodustat已进入临床阶段，来研究肾性贫血症。
货号:ajcx13078
CAS:1262132-81-9
分子式:C17H16N4O4
分子量：340.33
溶解度:DMSO: 83.33 mg/mL (244.85 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

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].

Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats[1].

[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.