| Bioactivity | Enarodustat is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat has the potential for renal anemia treatment. | ||||||||||||
| Target | EC50: 0.22 μM (factor prolyl hydroxylase) | ||||||||||||
| Invitro | Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible 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]. | ||||||||||||
| 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]. | ||||||||||||
| Name | Enarodustat | ||||||||||||
| CAS | 1262132-81-9 | ||||||||||||
| Formula | C17H16N4O4 | ||||||||||||
| Molar Mass | 340.33 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
Enarodustat
CAS: 1262132-81-9 F: C17H16N4O4 W: 340.33
Enarodustat is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μ
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