2009343-14-8

2009343-14-8 structure

Name: PHD-1-IN-1
Chemical Name: PHD-1-IN-1
CAS Number: 2009343-14-8
Molecular Formula: C₁₃H₈N₄
Molecular Weight: 220.23
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2020-06-02 00:06:41
Modify Date: 2024-01-10 11:40:45
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].

Name	PHD-1-IN-1

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.

Molecular Formula	C₁₃H₈N₄
Molecular Weight	220.23