JTZ-951(Enarodustat) Datasheet DC Chemicals
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Cat.No DC11607
Name JTZ-951(Enarodustat)

Chemical Properties

CAS 1262132-81-9
Formula C17H16N4O4
MW 340.339
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description
Target: EC50: 0.22 μM (factor prolyl hydroxylase)[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].
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].
Kinase Assay
Cell Assay
Animal Administration

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.
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