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” pocke
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
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Product Description
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.
IC50& Target:IC50: 0.034 μM (PHD-1)
Names and Identifiers
Smiles
N#CC1=CC=C(C2=CC=CC3=NC=NN23)C=C1
Molecular Weight
220.23
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