| Identification | Back Directory | [Name]
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- | [CAS]
2009343-14-8 | [Synonyms]
PHD-1-IN-1
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- | [Molecular Formula]
C13 H8 N4 | [MDL Number]
MFCD34470407 | [MOL File]
2009343-14-8.mol | [Molecular Weight]
220.23 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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]. | [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.
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| [storage]
Store at -20°C | [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. |
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