中文名:Enarodustat (JTZ-951)
英文名:Enarodustat (JTZ-951)
纯度:Moligand™,≥98%
货号:E414445
Cas号:1262132-81-9
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
Information
Enarodustat (JTZ-951) 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 (Cell-free assay); EPO release from Hep3B cells (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.
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.
Cell Research(from reference)
Cell lines:Hep3B cells
Incubation Time:24 h
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关键字: 伊那司他 (JTZ-951);C17H16N4O4 ; Glycine, N-((7-hydroxy-5-(2-phenylethyl)(1,2,4)triazolo(1,5-a)pyridin-8-yl)carbonyl)- ; JSK7TUA223
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