| Company Name: |
Shanghai YuanYe Biotechnology Co., Ltd.
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| Tel: |
021-61312847; 18021002903 |
| Email: |
3008007409@qq.com |
| Products Intro: |
Product Name:PHD-1-IN-1
CAS:2009343-14-8
Purity:98% Package:2mg Remarks:S23240
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| Company Name: |
Shanghai SuperLan Chemcial Technique Centre
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| Tel: |
0-2022843681 15618226720 |
| Email: |
chaolaichem@foxmail.com |
| Products Intro: |
Product Name:PHD-1-IN-1
CAS:2009343-14-8
Purity:95% Package:1G,5G,10G,50G,100G,1KG
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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](CAS/20200515/GIF/2009343-14-8.gif) |
| | 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 |
| | Benzonitrile, 4-[1,2,4]triazolo[1,5-a]pyridin-5-yl- Usage And Synthesis |
| 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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| | 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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