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| Cas No.: | 2009343-14-8 |
| Chemical Name: | PHD-1-IN-1 |
| Synonyms: | PHD-1-IN-1;PHD-1-IN-1 |
| SMILES: | N#CC1=CC=C(C2=CC=CC3=NC=NN23)C=C1 |
| Formula: | C13H8N4 |
| M.Wt: | 220.2 |
| Purity: | >98% |
| Sotrage: | -20 |
| Publication: | [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. |
| 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]. |
| 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. |
MSDS
COA
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| 2018-0101 |
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