PHD-1-IN-1 |
Catalog No.GC64584 |
PHD-1-IN-1은 IC50이 0.034μM인 경구 활성 및 강력한 HIF 프롤릴하이드록실라제 도메인-1(PHD-1) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2009343-14-8
Sample solution is provided at 25 µL, 10mM.
PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe2+ ion and induces the formation of an "Arg367-out" pocket[1].
PHD-1-IN-1 (compound 17; 3 mg/kg of p.o. or 0.5 mg/kg of i.v.) has a Cmax of 0.8 μM, a AUC of 176 ng•h/mL, Kp,uu of 1.11 and B/P of 0.95[1].
[1]. Ahmed S, et al. 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction. J Med Chem. 2017 Jul 13;60(13):5663-5672.
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