1262132-81-9

1262132-81-9 structure

Name: JTZ-951
Chemical Name: enarodustat
CAS Number: 1262132-81-9
Molecular Formula: C₁₇H₁₆N₄O₄
Molecular Weight: 340.333
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2018-09-01 17:41:19
Modify Date: 2024-01-09 11:54:52
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.

Name	enarodustat
Synonyms	JSK7TUA223 enarodustat Glycine, N-[[7-hydroxy-5-(2-phenylethyl)[1,2,4]triazolo[1,5-a]pyridin-8-yl]carbonyl]- N-{[7-Hydroxy-5-(2-phenylethyl)[1,2,4]triazolo[1,5-a]pyridin-8-yl]carbonyl}glycine

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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase Research Areas >> Others
Target	EC50: 0.22 μM (factor prolyl hydroxylase)[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].
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].
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.