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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Enarodustat (JTZ-951)
CAS number：1262132-81-9 molecular formula：C17H16N4O4
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| Chinese alias | 伊那司他 (JTZ-951) | ||
| English alias | C17H16N4O4 | Glycine, N-((7-hydroxy-5-(2-phenylethyl)(1,2,4)triazolo(1,5-a)pyridin-8-yl)carbonyl)- | JSK7TUA223 | UNII-JSK7TUA223 | Enarodustat (JTZ-951) | JTZ 951 | HY-109057 | BJ162590 | DB14985 | EX-A4798 | MS-25187 | 2-(7-Hydroxy-5-phenethyl-[1,2,4]tr | ||
| CAS number | 1262132-81-9 | molecular formula | C17H16N4O4 |
| molecular weight | 340.33 g/mol | Exact mass | - |
| PSA | 111.000 Ų | logp | 1.511 |
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