Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Egl nine homolog 1 inhibitor
Product Description
Information
Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. Enarodustat has the potential for the treatment of renal anemia.
Enarodustat (JTZ-951) inhibits PHD2 with IC50 of 0.22 μM and the EPO release from Hep3B cells with EC50 of 5.7 μM.
In vivo
JTZ-951 (compound 14), with a 5-phenethyl substituent on the triazolopyridine group, increases hemoglobin levels with daily oral dosing in rats. JTZ-951 is rapidly absorbed after oral administration and disappears shortly thereafter, which can be advantageous in terms of safety. JTZ-951 is selected as a clinical candidate.
1.Sanford M, McCormack PL. (2017) Erratum Regarding "Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD" (Am J Kidney Dis. 2017;69[6]:815-826).. Am J Kidney Dis, 69 (6):(869). [PMID:28532635][10.1021/op500134e]
2.Markham A. (2021) Enarodustat: First Approval.. Drugs, 81 (1):(169-174). [PMID:33320297][10.1021/op500134e]
3.Ogoshi Y, Matsui T, Mitani I, Yokota M, Terashita M, Motoda D, Ueyama K, Hotta T, Ito T, Hase Y et al.. (2017) Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.. ACS Med Chem Lett, 8 (12):(1320-1325). [PMID:29259755][10.1021/op500134e]
4.Fukui K, Shinozaki Y, Kobayashi H, Deai K, Yoshiuchi H, Matsui T, Matsuo A, Matsushita M, Tanaka T, Nangaku M. (2019) JTZ-951 (enarodustat), a hypoxia-inducibe factor prolyl hydroxylase inhibitor, stabilizes HIF-α protein and induces erythropoiesis without effects on the function of vascular endothelial growth factor.. Eur J Pharmacol, 859 (13):(172532). [PMID:31301309][10.1021/op500134e]
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