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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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.
|Related HIF Products|
LW6 is a novel HIF-1alpha inhibitor, with an IC50 of 4.4 μM.
PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
JNJ-42041935 is a potent, competitive, reversible, and selective inhibitor of PHD with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09 for PHD1, PHD2, and PHD3, respectively.
Daprodustat (GSK1278863) is a novel, orally active HIF-prolyl hydroxylase inhibitor.
BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD) with IC50 of 3.9 uM for PDH2 enzyme.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.