| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.034 μM (PHD-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: | ||||||||||||
| Name | PHD-1-IN-1 | ||||||||||||
| CAS | 2009343-14-8 | ||||||||||||
| Formula | C13H8N4 | ||||||||||||
| Molar Mass | 220.23 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
PHD-1-IN-1
CAS: 2009343-14-8 F: C13H8N4 W: 220.23
PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PH
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