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JTZ-951(Enarodustat)

  Cat. No.:  DC11607   Featured
Chemical Structure
1262132-81-9
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More than 5000 active chemicals with high quality for research!
Field of application
A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
Cas No.: 1262132-81-9
Chemical Name: Enarodustat
Synonyms: JTZ 951;JTZ951;Enarodustat
SMILES: C(O)(=O)CNC(C1=C(O)C=C(CCC2=CC=CC=C2)N2N=CN=C12)=O
Formula: C17H16N4O4
M.Wt: 340.34
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia.
Target: EC50: 0.22 μM (factor prolyl hydroxylase)[1]
In Vivo: Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats[1].
In Vitro: Enarodustat (JTZ-951) is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat exhibits neither CYP (IC50 > 100 μM; CYP3A4/5, CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2C8, CYP2B6) nor hERG (IC50 > 100 μM) inhibition[1].
References: [1]. Ogoshi Y, et al. Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia. ACS Med Chem Lett. 2017 Nov 20;8(12):1320-1325.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC11607 JTZ-951(Enarodustat) A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
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