JTZ-951

Names

[ Name ]:
JTZ-951

[Synonym ]:
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

Biological Activity

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₁₇H₁₆N₄O₄

[ Molecular Weight ]:
340.333

[ Exact Mass ]:
340.117157

[ LogP ]:
1.60

[ Index of Refraction ]:
1.690

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.