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PHD-1-IN-1

Names

[ CAS No. ]:
2009343-14-8

[ Name ]:
PHD-1-IN-1

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

[Target]

IC50: 0.034 μM (PHD-1)[1]


[In Vivo]

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]. Animal Model: Male C57BL6 mice[1] Dosage: 3 mg/kg (p.o.) or 0.5 mg/kg (i.v.) (Pharmacokinetic Analysis) Administration: PO or IV Result: Had a Cmax of 0.8 μM, a AUC of 176 ng•h/mL, Kp,uu of 1.11 and B/P of 0.95.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C13H8N4

[ Molecular Weight ]:
220.23

Related Compounds