Home Angiogenesis HIF inhibitor Enarodustat (JTZ-951)

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Enarodustat (JTZ-951) HIF inhibitor

Cat.No.S9656

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. It has the potential for the treatment of renal anemia.
Enarodustat (JTZ-951) HIF inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 340.33

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (199.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2.5 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 340.33 Formula

C17H16N4O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1262132-81-9 -- Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O

Mechanism of Action

Targets/IC50/Ki
PHD2
(Cell-free assay)
0.22 μM
EPO release from Hep3B cells
(Cell-based assay)
5.7 μM(EC50)
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.
In vivo

Enarodustat (JTZ-951), with a 5-phenethyl substituent on the triazolopyridine group, increases hemoglobin levels with daily oral dosing in rats. It is rapidly absorbed after oral administration and disappears shortly thereafter, which can be advantageous in terms of safety. This compound is selected as a clinical candidate.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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