JTZ-951

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型有效的口服活性 HIF 脯氨酰羟化酶 (PHD) 抑制剂，对 PHD2 的 IC50 为 0.22 uM。

A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2; increases EPO release from Hep3B cells with EC50 of 5.7 uM, increases hemoglobin levels in rats.Anemia Phase 2 Clinical(In Vitro):Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible 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.(In Vivo):Enarodustat (1 and 3 mg/kg, p.o.) increases hemoglobin levels in a dose-dependent manner with daily oral dosing in rats.

Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible 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.

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

JTZ 951 | JTZ951 | Enarodustat

Angiogenesis

HIF/HIF Prolyl-hydroxylase

HIF/HIF Prolyl-hydroxylase

Other Indications

Anemia

1262132-81-9

340.339

C17H16N4O4

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (244.85 mM)

O=C(O)CNC(C1=C(O)C=C(CCC2=CC=CC=C2)N3C1=NC=N3)=O

(7-hydroxy-5-phenethyl-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)glycine

(-20℃)

With Ice Pack

≥ 2 years