ChemicalBook >> CAS DataBase List >>Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-
- CAS No.
- 2009343-14-8
- Chemical Name:
- Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-
- Synonyms
- PHD-1-IN-1;Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-;pocket,ion,Arg367-out,HIF-PH,Hypoxia-inducible factors,site,active,PHD 1 IN 1,orally,Inhibitor,PHD-1,Fe2+,PHD1IN1,iron,HIF/HIF Prolyl-Hydroxylase,HIFs,inhibit
- CBNumber:
- CB35954015
- Molecular Formula:
- C13 H8 N4
- Molecular Weight:
- 220.23
- MDL Number:
- MFCD34470407
- MOL File:
- 2009343-14-8.mol
Last updated:2024-07-02 08:55:06
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Chemical Properties,Uses,Production
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].
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.
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Preparation Products And Raw materials
Raw materials
Preparation Products
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Suppliers
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Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-
PHD-1-IN-1
pocket,ion,Arg367-out,HIF-PH,Hypoxia-inducible factors,site,active,PHD 1 IN 1,orally,Inhibitor,PHD-1,Fe2+,PHD1IN1,iron,HIF/HIF Prolyl-Hydroxylase,HIFs,inhibit
2009343-14-8