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” pocket
In Vivo
PHD-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.
Form:Solid
IC50& Target:IC50: 0.034 μM (PHD-1)
规格
规格或纯度
≥99%
英文名称
PHD-1-IN-1
生化机理
PHD-1-IN-1 是一种具有口服活性的强效 HIF 丙氨酰羟化酶结构域-1(PHD-1)抑制剂,其 IC 50 为 0.034 μM。PHD-1-IN-1 与活性位点的 Fe 2+ 离子具有独特的单齿结合相互作用,并诱导形成 "Arg367-out "卵巢。