Enarodustat (JTZ-951)

Catalog No.S9656 Batch:S965601

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Technical Data

Formula

C17H16N4O4
Molecular Weight 340.33 CAS No. 1262132-81-9
Solubility (25°C)* In vitro DMSO 68 mg/mL (199.8 mM)
Ethanol 2.5 mg/mL (7.34 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Male balb/c mice, CD (SD) rats

  • Dosages

    1 mg/kg, 3 mg/kg

  • Administration

    Oral gavage

Selleck's Enarodustat (JTZ-951) has been cited by 1 publication

CIRP attenuates acute kidney injury after hypothermic cardiovascular surgery by inhibiting PHD3/HIF-1α-mediated ROS-TGF-β1/p38 MAPK activation and mitochondrial apoptotic pathways [ Mol Med, 2023, 29(1):61] PubMed: 37127576

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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