JTZ-951

Modify Date: 2024-01-09 11:54:52

JTZ-951 Structure
JTZ-951 structure
Common Name JTZ-951
CAS Number 1262132-81-9 Molecular Weight 340.333
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C17H16N4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of JTZ-951


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.

 Names

Name enarodustat
Synonym More Synonyms

 JTZ-951 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
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.

 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

 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