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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. Enarodustat has the potential for the treatment of renal anemia.
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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 DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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

Read more about storage stability stock solution CAS number SMILES

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 2025-07-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06725810 RECRUITING
Chronic Kidney Disease Associated Anemia
Shanghai Zhongshan Hospital
2025-03-27 PHASE4
NCT07522996 WITHDRAWN
Transfusion-dependent Non-severe Aplastic Anemia
Peking Union Medical College Hospital
2026-06 PHASE3
NCT07548671 NOT_YET_RECRUITING
Transfusion-dependent Non-severe Aplastic Anemia
Peking Union Medical College Hospital
2026-04 PHASE3
NCT07079579 NOT_YET_RECRUITING
Renal Anemia in Non-dialysis Chronic Kidney Disease
Shenzhen Salubris Pharmaceuticals Co., Ltd.
2025-08 PHASE4
NCT06737081 RECRUITING
Anemia
Shenzhen Salubris Pharmaceuticals Co., Ltd.
2024-09-14 PHASE2
NCT04027517 COMPLETED
Anemia of Chronic Kidney Disease
JW Pharmaceutical
2019-01-15 PHASE3

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