PHD-1-IN-1

Modify Date: 2024-01-10 11:40:45

PHD-1-IN-1 Structure
PHD-1-IN-1 structure
Common Name PHD-1-IN-1
CAS Number 2009343-14-8 Molecular Weight 220.23
Density N/A Boiling Point N/A
Molecular Formula C13H8N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PHD-1-IN-1


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].

 Names

Name PHD-1-IN-1

 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
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
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