Home Angiogenesis HIF inhibitor Enarodustat (JTZ-951) For research use only.

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) Chemical Structure

Enarodustat (JTZ-951) Chemical Structure

CAS No. 1262132-81-9

Purity & Quality Control

Batch: S965601 DMSO]68 mg/mL]false]Ethanol]2.5 mg/mL]false]Water]Insoluble]false Purity: 99.95%
99.95

Enarodustat (JTZ-951) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Biological Activity

Description 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.
Targets
PHD2 [1]
(Cell-free assay)		 EPO release from Hep3B cells [1]
(Cell-based assay)
0.22 μM 5.7 μM(EC50)
In vitro
In vitro

Enarodustat (JTZ-951) inhibits PHD2 with IC50 of 0.22 μM and the EPO release from Hep3B cells with EC50 of 5.7 μM.[1]
Cell Research Cell lines Hep3B cells
Concentrations --
Incubation Time 24 h
Method

Human Hep3B cells are inoculated into 96-well flat-bottomed plates and on the next day, each test compound is added at appropriate concentrations for the assessment of EPO production. The culture supernatants are collected at 24 hours after the addition of each of the test compounds. A hypoxic condition is established and the EPO concentration of this condition is defined as 100% when the EC50 is calculated. The EPO concentration in culture supernatants is measured by human EPO ELISA kit.
In Vivo
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]
Animal Research Animal Models Male balb/c mice, CD (SD) rats
Dosages 1 mg/kg, 3 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02805244 Completed
Anemia of Chronic Kidney Disease
Akros Pharma Inc.
 June 2016 Phase 1
NCT01978587 Completed
Anemia in Chronic Kidney Disease
Akros Pharma Inc.
 October 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 340.33 Formula

C17H16N4O4
CAS No. 1262132-81-9 SDF --
Smiles C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 68 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2.5 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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