Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-

Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Suppliers list
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Products Intro: Product Name:PHD-1-IN-1
CAS:2009343-14-8
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CAS:2009343-14-8
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Products Intro: Product Name:PHD-1-IN-1
CAS:2009343-14-8
Purity:98% HPLC Package:5mg，10mg，50mg，100mg，1g，5g
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Products Intro: Product Name:PHD-1-IN-1
CAS:2009343-14-8
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Products Intro: Product Name:PHD-1-IN-1
CAS:2009343-14-8
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Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Basic information
Product Name:Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl-
Synonyms: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;4-([1,2,4]Triazolo[1,5-a]pyridin-5-yl)benzonitrile;PHD-1-IN-1, 10 mM in DMSO
CAS:2009343-14-8
MF:C13 H8 N4
MW:220.23
EINECS:
Product Categories:
Mol File:2009343-14-8.mol
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Structure
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Chemical Properties
storage temp. Store at -20°C
solubility DMSO : 195 mg/mL (885.44 mM; Need ultrasonic)
form Solid
color White to off-white
Safety Information
MSDS Information
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Usage And Synthesis
UsesPHD-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 ActivityPHD-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 ngh/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 ngh/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 ngh/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.
Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Preparation Products And Raw materials
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