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JTZ-951

Cat. No. M9198
JTZ-951 Structure
Synonym:

Enarodustat

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Enarodustat (JTZ-951) exhibits neither CYP (IC50 > 100 μM; CYP3A4/5, CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2C8, CYP2B6) nor hERG (IC50 > 100 μM) inhibition. 

In vivo, Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 340.33
Formula C17H16N4O4
CAS Number 1262132-81-9
Purity >98%
Solubility DMSO
Storage at -20°C
References

Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.
Ogoshi Y, et al. ACS Med Chem Lett. 2017 Nov 20;8(12):1320-1325. PMID: 29259755.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JTZ-951, Enarodustat supplier, HIF, inhibitors

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