PHD-1-IN-1 (C007B-386689)

PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC 50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an “Arg367-out” pocketIn VivoPHD-1-IN-1 (compound 17; 3 mg/kg of p.o. or 0.5 mg/kg of i.v.) has a C max of 0.8 μM, a AUC of 176 ng•h/mL, K p,uu of 1.11 and B/P of 0.95 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL6 mice Dosage: 3 mg/kg (p.o.) or 0.5 mg/kg (i.v.) (Pharmacokinetic Analysis) Administration: PO or IV Result: Had a C max of 0.8 μM, a AUC of 176 ng•h/mL, K p,uu of 1.11 and B/P of 0.95.IC50& Target:IC50: 0.034 μM (PHD-1). Specification: 10mM in DMSO Molecular Formula: C13H8N4 Molecular Weight: 220.23